Cambridge University Press
0521770971 - Modern Methods of Organic Synthesis - by W. Carruthers and Iain Coldham
Index



Index




acidity 1

acyl anion equivalents 56

acyloin reaction 425

Adams’ catalyst 407

AD-mix α 352

AD-mix β 352

agelastatin A 376

AIBN 268

alane 437, 444

alcohols

   deoxygenation 270

   from alkenes 323, 349

   from carbonyl compounds 416, 421, 423, 434–56

   oxidation 378–93

aldehydes

   alkylation of 17

   as dienophiles in Diels–Alder reaction 169

   decarbonylation of 419

   from alcohols 380

   from alkenes 325, 360, 364

   oxidation of 392

   reduction of 435, 439, 443

   reductive dimerization of 148, 425

Alder–ene reaction 231

aldol reaction 27–36

   diastereoselective 32

   enantioselective 41

aldosterone 276

alkenes

   allylic oxidation of 374

   conversion to alcohols 323

   conversion to ketones (Wacker reaction) 365

   epoxidation of 331–46

   hydroboration of 315–30

   oxidation to diols 349–57

   oxidative cleavage of 360

   ozonolysis of 360

   preparation of

     by elimination reactions 105, 111

     by fragmentation reactions 118

     by metathesis reactions 151

     by Wittig and related reactions 132–43

     from alkenyl phosphates 433

     from alkynes 125–32

     from diols 123

     from hydrazones 120

   reaction of

     with carbenes 303–9

     with dienes in Diels–Alder reaction 162

     with radicals 280–98

   reduction of 322, 408–13, 459

alkenyllithium species 57, 59

alkylation 1–19

   asymmetric 37

   with enamines 1, 17

   with enolates 1–16

   with metalloenamines 16

alkyl halides

   oxidation to carbonyl compounds 384

   reductive cleavage to hydrocarbons 269, 406, 442

alkyllithium species 46

alkynes

   conversion to alkenes 125–32, 414

   deprotonation of 58

   hydrometallation 128

   preparation of 137

   reduction of 125

allopumiliotoxin 58

allosamidin disaccharides 272

allylic organometallics 71–4

allylic oxidation 374

allylic 1,3-strain 26, 73, 351

π-allylpalladium complexes 98

amabiline 220

ambruticin S 308

amino-hydroxylation 358

anionic oxy-Cope rearrangement 241

apovincamine 431

Arbuzov reaction 138

Arndt–Eistert method 309

aspidosperma alkaloids 199

asymmetric reactions

   aldol reaction 41

   alkylation of enolates 37

   allylation of carbonyl compounds 74

   allylic oxidation 376

asymmetric reactions (cont.)

   cycloaddition reactions 183, 202–11, 218, 226

   cyclopropanation 305, 307

   dihydroxylation 352–5

   ene reactions 233

   epoxidation 337–46

   epoxide-opening 109

   hydroboration 321

   hydrogenation 420

   organo-catalytic 45, 397

   oxidation of alcohols (kinetic resolution) 389

   palladium-catalyzed 96, 100

   radical reactions 281

   reduction of alkenes 420

   reduction of ketones 421, 452

   with chiral organolithium compounds 50

   with enzymes 355, 371, 401, 454

avarone 373

avenaciolide 216

aza-Cope rearrangement 242

aziridination 346

azomethine ylides 228

Baeyer–Villiger reaction 398

bafilomycin A1 385

balanol 297

Bamford–Stevens reaction 120, 300

Barton decarboxylation 271

Barton deoxygenation 271

Barton reaction 276

Baylis–Hillman reaction 31

9-BBN 317

Beckmann rearrangement 277

benzene derivatives

   Birch reduction of 429

   hydrogenation of 414

   oxidation of 355, 371

benzocyclobutenes 181, 260

benzoin condensation 57

benzoquinones 164, 181, 191, 208, 373

benzylidene acetal, reductive cleavage 462

benzynes 5, 166

Bergman cycloaromatization reaction 147

BINAP 96, 420

BINOL 74, 208, 233

biotransformations 355, 371, 401, 454

Birch reduction 427, 430

9-borabicyclo[3.3.1]nonane see 9-BBN

borane 449

boron enolates 30, 33, 42, 88, 250

Bouveault–Blanc 425

brefeldin 60, 253

brevetoxin B 136

brevicomin 120, 281, 314

BRL-55834 343

Bürgi–Dunitz angle 36

calicheamicins 94, 224, 251

calyculin A 320

camptothecin 291

CAN 373

capnellene 236, 263

carbenes 85, 299–311

carbenoids 299

carboalumination of alkynes 132

carbocupration of alkynes 131

carbolithiation 49

carbonyl ylides 230

Caro’s acid 398

carvone 188

caryophyllene 212

catecholborane 319

CC-1065 292

cedrene 295

cerium trichloride 47, 438

cerulenin 217

cervinomycin A 262

chelation control 64

cheletropic reaction 272–304

ChiraPHOS 420

chloramine-T 347, 358

m-chloroperoxybenzoic acid see mCPBA

N-chlorosuccinimide 273, 383

chromic acid 370, 371, 378, 392

chromium trioxide 378

Chugaev reaction 113

cis-principle, in Diels–Alder reaction 189

Claisen condensation 11, 30

Claisen rearrangement 244–52

Clemmensen reduction 426

cobalt-mediated cyclization 86

Collins’ reagent 376, 380

combretastatin A-1 156

compactin 178

complex induced proximity effect 60

conduramine 173

conduritol A 200

Conia reaction 237

coniceine 152, 285

conjugate addition 19–27, 40, 66, 76

conessine 275

Cope elimination 113

Cope rearrangement 239–43

Corey–Fuchs reaction 137

Corey–Kim oxidation 383

Corey–Winter reaction 124

coriolin 87

Cram’s rule see Felkin–Anh model

cross-metathesis 154

cryptone 321

cycloaddition reactions

   [2+2] 211

   [2+2+2] 89

   [4+2] see Sections 3.1, 3.3, 3.4

   Diels–Alder 159–211

   dipolar 222–31

   with allyl anions and cations 219–21

cyclocitral 256

cycloeudesmol 308

cyclopropanes

   from carbenes 304

   from sulfoxonium ylides 54

cyclotrimerization 89

cytovaricin 102

dactylol 153

Dakin reaction 401

Danishefsky’s diene 170, 176

daphniphyllum alkaloids 197

daunoomycinone 182

DBU 109

DDQ 373

decarbonylation 419

decarboxylation 6

decarestrictine L 257

Dess–Martin reagent 389

DHQ and DHQD 352

dianions 10

diazocarbonyl compounds 53, 230, 257, 299, 300, 303, 306–11

DIBAL-H 437, 445

dichloromethyllithium 328

Diels–Alder reaction 159–211

   asymmetric 202

   intramolecular 193

   regioselectivity 185

   retro-Diels–Alder 199

   stereoselectivity 188

dienes 174–85

dienophiles 162–74

diethylzinc 70

dihydroquinidine see DHQD

dihydroquinine see DHQ

dihydrosterculic acid 305

dihydroxylation of alkenes 349–57

di-imide 459

di-isopinocampheylallyl borane 74

di-isopinocampheylborane 321

di-isopinocampheylboron triflate 43

di-isopinocampheylchloroborane 453

dimethylsulfonium methylide 53

dimethylsulfoxonium methylide 53

diolmycin 341

1,2-diols, preparation from alkenes 349–57

DIOP 420

dioxiranes 336, 344

DIPAMP 420

dipolar cycloaddition reactions 222–31

diplodialide A 11

dipolarophiles 222

disiamylborane 316

disodium prephenate 176

dithianes 56

DMDO 336

Dötz reaction 85

DuPHOS 420

dynemicin A 94

ecdysone 99

echinocandin D 326

electrocyclic reactions 259

elimination reactions

   β-eliminations 105–10

   pyrolytic syn eliminations 111

enamines 17, 22

ene reaction 231–8

enediynes 94, 147

enolates

   aldol reaction with 28–36

   alkylation with 2–11

   conjugate addition with 19–27

   regioselective formation of 7, 12, 14, 16

   stereoselective formation of 14, 33, 248

enol ethers, α-lithiation 57

enols 2

enol silanes see silyl enol ether

enol triflates 80, 90, 91, 93, 97

enone formation 394

enzymes see biotransformations

EO9 373

epibatidine 270, 388, 439

epothilones 153

epoxidation 331–46

epoxides

   from alkenes 331–46

   from sulfur ylides 53, 310

   ring-opening 67, 81, 109, 442

ergosterol 173

Eschenmoser fragmentation 120

Eschenmoser’s salt 110

Eschweiler–Clark reaction 447

estradiol 198

estrone 260

Étard reaction 372

Evans aldol reaction 42

Felkin–Anh model 36, 47, 69, 440

Fetizon’s reagent 386

Fischer carbenes 85

Fischer indole synthesis 251

FK-506 55, 271

formamidines 49

FR-900848 305

FR-901464 128, 211

fragmentation reactions 118–20

fredericamycin A 464

free radical reactions 268–98

Fremy’s salt 373

frondosin B 264

galanthamine 385

gephyrotoxin 172

germacrane sesquiterpenes 242

Gilman reagents 75

Glaser reaction 94

glutathione 433

grandisol 369

grayanotoxin 293

Grignard reagents 67

Grob fragmentation 118

Grubbs catalyst 151

halichlorine 329

halogen–lithium exchange 46, 49, 59, 62

halogen–magnesium exchange 63

Heck reaction 94

hemibrevetoxin B 110

hennoxazole A 146

heterodienes in Diels–Alder reaction 183

hetereodienophiles in Diels–Alder reaction 169

hirsutene 290

histrionicotoxin 390

Hofmann–Löffler–Freytag reaction 273

Hofmann reaction 107

Hofmann rule in eliminations 106

Horner–Wadsworth–Emmons reaction 138

Horner–Wittig reaction 140

hybocarpone 264

hydrazones 19

hydroalumination 129

hydroboration

   of alkenes 316–30

   of alkynes 127

hydrogenation 405–22

hydrogenolysis 406

hydrosilylation 131

hydrostannylation 131

α-hydroxy-ketones 396

hydrozirconation 128

hyellazole 262

hypervalent iodine reagents 374, 389, 395, 397

ibogamine 208

IBX 372, 389, 396

indanomycin 194

indinavir 368

indolizidines 227

iodic acid 396

N-iodosuccinimide 278

ipsdienol 234

Ireland–Claisen rearrangement 248

iridomyrmecin 25

isocaryophyllene 149

isocomene 213, 308

Jacobsen–Katsuki epoxidation 342

jasmone 58, 103

Johnson–Claisen rearrangement 245

Jones’ reagent 378

juglone 373

Julia olefination 144

juvabione 242

juvenile hormone 118, 130

kainic acid 235, 292

kallolide B 253

kamausallene 293

kempene-2 148

ketenes 216

ketones

   alkylation of 7

   from alcohols 378–92

   from alkenes 325, 327, 360, 365

   from alkynes 323

   oxidation of 394–401

   reduction of

     to alcohols 416, 421, 423, 434–56

     to methylene compounds 426, 448, 457, 458, 462

   reductive dimerization of see pinacol reaction

Kharasch–Sosnovsky reaction 376

khusimone 236

kinetic enolate formation 8, 12, 29, 33

kinetic resolution

   of allylic alcohols 340

   of benzylic alcohols 389

   of epoxides 343

Knoevenagel condensation 30

Kuhn–Roth estimation 370

Kulinkovich reaction 65

lactones

   from ketones by Baeyer–Villiger reaction 398

   reduction of, to lactols 445

laulimalide 341

lavendamycin 201

lennoxamine 297

Lewis acids

   in addition to aldehydes 68, 70, 73

   in aldol reaction 29

   in alkylation 13

   in conjugate addition 23, 76

   in Diels–Alder reaction 169, 187

   in ene reaction 231

   in epoxide opening 442

   in reductions 438, 462

linalool 259

Lindlar’s catalyst 125, 414

lipstatin 218

lithium aluminium hydride 435

   modification of reducing properties by

     alcohols 443

     aluminium chloride 444

lithium diisopropylamide (LDA) 6

lithium hexamethyldisilazide (LHMDS) 6

lividosamine 223

Lombardo reagent 150

L-selectride 441

Luche reduction 438

luciduline 227

lupinine 197

lycoricidine 172

malyngolide 302

manganese dioxide 384

Mannich reaction 110, 242

manzamine A 196, 214

McMurry reaction 123, 148, 425

mCPBA 331, 398

Meerwein–Pondorff–Verley reduction 434

Meisenheimer rearrangement 259

mesembrine 22, 303

metallocarbenes 299

metalloenamines 19

metallo-ene reaction 235

metathesis of alkenes 151–4

methyl chrysanthemate 155

methyltrioxorhenium 335

Michael reaction 20

minovine 165

Mitsunobu reaction 4

molecular orbital theory

   in Diels–Alder reaction 160

mono-isopinocampheylborane 321

MonoPhos 421

MoOPH 396

morphine 292

Mukaiyama aldol reaction 29, 44

muscarine 301

myrtanol 324

naproxen 98, 421

Nazarov cyclization 263

Nef reaction 58

Negishi reaction 69

nemorensic acid 431

Newman projection 36, 47, 64

Nicholas reaction 88

nicotine 367

nitrenes 347

nitrile oxides 223

nitrones 225

nitrosobenzene 397

NMO 350, 387

nonactic acid 221

Nozaki–Hiyama–Kishi reaction 84

oestrone 425

Oppenauer oxidation 392

organoborane compounds 315

organo-catalysis 26, 45, 397

organochromium reagents 81–5, 150, 217, 306

organocobalt reagents 85–9

organocopper reagents 75–81, 131

organolithium species 45–63

organomagnesium reagents 63–7

organomercury compounds 272, 285, 295

organopalladium species 89–101

organozinc reagents 67–71

ortho-lithiation 60

ortho-quinodimethanes 181, 198, 260

Oshima–Lombardo reagent 150

osmium tetroxide 349

Overman rearrangement 252

oxaphosphetane 133

oxazaborolidine 453

oxaziridines 337, 396

oxaziridinium salts 337

oxidation

   of aldehydes 392

   of alkanes 370

   of alkenes 374

   of benzenes 371

   of alcohols 378–93

   of ethers 393

   of ketones 394

oxidative cleavage of alkenes 360–4

Oxone® 324, 364

oxy-Cope rearrangement 240

ozonolysis 222, 360

paeonilactone A 80

palladium complexes

   π-allyl 98

   in coupling reactions 89–101

   in metallo-ene reaction 101, 238

   in oxidation of alkenes 365

   in [3,3]-sigmatropic rearrangements 239, 252

palladium-ene reaction 101, 238

pancracine 243

pancratistatin 252, 355

parviflorin 353

Paternò–Büchi reaction 215

Pauson–Khand reaction 86

PCC 376, 380

PDC 380, 393

penicillins 256

pentalenene 366

perhydrohistrionicotoxin 277

pericyclic reactions 159

periodic acid 393

periplanone-B 142

peroxy acids 331, 398

Petasis reagent 149

Peterson reaction 141

phorboxazole B 462

phosphonium ylides 133

photocycloadditions 211

photolysis 268, 271, 276, 300, 310

phyllodulcin 63

physostigmine 96

phytuberin 363

pinacol reaction 148, 425

pinnaic acid 156

pKa values 1

plicamine 374

podocarpic acid 294

polymer-supported catalysts and reagents 355, 374, 386, 388, 439

polymethylhydrosiloxane (PMHS) 461

potassium permanganate 349, 356, 371, 385

precapnelladiene 214

preussin 215

Prévost reaction 357

prostaglandins 48, 92, 246, 290, 400

pumiliotoxin C 177, 463

pyridinium chlorochromate see PCC

pyridinium dichromate see PDC

pyrolytic eliminations 111

quinidine 31, 218, 250

quinuclidine 31

quinones 164, 373

radicals 268–98

Ramberg–Bäcklund reaction 146

Raney nickel 52, 407, 415, 458

rearrangements

   of carbocations 107

   of sulfoxides 258

   see also sigmatropic rearrangements

reduction

   asymmetric 420, 452, 455

   dissolving metal 422

   of acetals 462

   of acid chlorides 443, 460

   of aldehydes and ketones 416, 423, 434, 437, 448, 451, 461

   of alkenes 408, 459

   of alkyl halides 270, 406, 442

   of alkynes 125, 414, 432

   of aromatics 414, 429

   of carboxylic acids 435, 450

   of carboxylic amides 435, 444, 445, 451

   of enones 427, 438, 461

   of epoxides 442, 452

   of esters 425, 435, 439, 444, 445, 460

   of imines 446

   of nitriles, oximes and nitro compounds 416, 444, 445

   of sulfonates 442

reductive amination 446

reductive cleavage reactions 432

Reformatsky reaction 68

reserpine 191

reticuline 50

retro Diels–Alder reaction 199

rhodium catalysts 14, 230, 301, 306, 310, 319, 321, 410, 415, 417, 420, 447

rifamycin 324

ring-closing metathesis 152

rishirilide B 182

Robinson annulation 26

Rosenmund reduction 460

ruthenium tetroxide 364, 394

SAE reaction see Sharpless asymmetric epoxidation

samarium diiodide 285, 293

sanglifehrin 37

santalene 168

sarcomycin 199, 224

sarcophytol 425

sarain A 228

Saytzeff elimination 106

Schlenk equilibrium 63

Schlosser’s base 46

Schrock catalyst 151

Schwartz reagent 128

scopadulcic acid A 240

secologanin 164

secondary orbital overlap 192

sedridine 225

selenium dioxide 374

selenoxides 116

self-regeneration of chirality

septorin 103

sesquicarene 308

Shapiro reaction 121

Sharpless asymmetric dihydroxylation 352

Sharpless asymmetric epoxidation 338

shikimic acid 178, 207

sigmatropic rearrangements

   [2,3] 253–9

   [3,3] 238–52

silver carbonate oxidation of alcohols 386

silyl enol ethers 11–14, 23, 29, 248, 460

Simmons–Smith cyclopropanation 272–304

slaframine 171

SN2 4, 79

sodium borohydride 435

sodium chlorite 393

sodium cyanoborohydride 446

sodium triacetoxyborohydride 447

solenopsin 225

Sommelet–Hauser rearrangement 257

Sonogashira reaction 93

sparteine 50, 389

squalene 52

Staudinger reaction 218

Stevens rearrangement 256

Still–Wittig reaction 140

Stille reaction 90

strychnine 41, 96, 243, 251

Stryker’s reagent 461

sulfones 55, 144, 166, 198, 284, 433

sulfoxides 115, 167, 177, 258

sulfur ylides 53, 310

Suzuki reaction 92, 329

Swern oxidation 382

TADDOL 208

Takai olefination 150

taxanes 194, 359, 387

tazettine 96

Tebbe reagent 149

tedanolide 394

TEMPO 391, 393

terpineol 204

tetra-n-propylammonium perruthenate see TPAP

thermodynamic enolate formation 8, 16, 21, 29

thexylborane 317

thienamycin 303

Thorpe–Ingold effect 288

tin–lithium exchange 51, 59

titanium reagents 29, 31, 34, 41, 44, 52, 58, 74, 123, 148, 208, 233, 338, 425

toxol 410

TPAP 387

transfer hydrogenation 406

trialkylsilanes as reducing agents 460

tributyltin hydride 188, 269, 270, 281, 288, 295

tris(trimethylsilyl)silane 284

tumerone 13

tylonolide 270

umpolung 56

unactivated C–H bonds, functionalization of 272–278

α,β-unsaturated carbonyl compounds

   alkylation of 15, 16

   as dienes in Diels–Alder reactions 164, 183

   as dienophiles in Diels–Alder reactions 162

   as dipolarophiles 226

   deconjugative alkylation of 14, 77

   in conjugate addition reactions 19–27, 40, 75

   in photocycloaddition with alkenes 211

   preparation by allylic oxidation 374, 376

   reduction to alkenes 433, 437, 438, 445, 446, 448, 458

   reduction to the saturated carbonyl compound 409, 410, 418, 420, 427, 461

Upjohn dihydroxylation 350

valerane 77

vanadium acetylacetonate 334

vancomycin 369

vernolepin 279

vitamin D 173, 179

Wacker oxidation reaction 365

Wadsworth–Emmons reaction 138

Weinreb amide 65

widdrol 249

Wilkinson’s catalyst 319, 417, 460

Wittig reaction 132–41

Wittig rearrangement 253

Wolff–Kishner reduction 457

Wolff rearrangement 309

Woodward–Hoffmann rules 160, 192, 219, 259

Woodward–Prévost reaction 357

xanthates, in pyrolysis to give alkenes 111, 113

ylides

   phosphonium 133

   sulfonium 53, 310

Zaitsev elimination 106

zampanolide 157

zearalenone 90

Zimmerman–Traxler model 32, 41

zinc, as reducing agent 423, 426




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