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举例 :可输入Filippa Pettersson 或者 Cancer Res. 75(6) , 1102-12, (2015) 或者10.1002/anie.201600521

A practical synthesis of a γ-secretase inhibitor

…, CJ McWilliams, GW Stewart, RD Wilson…

文献索引：Scott, Jeremy P.; Lieberman, David R.; Beureux, Olivier M.; Brands, Karel M. J.; Davies, Antony J.; Gibson, Andrew W.; Hammond, Deborah C.; McWilliams, Chris J.; Stewart, Gavin W.; Wilson, Robert D.; Dolling, Ulf-H. Journal of Organic Chemistry, 2007 , vol. 72, # 11 p. 4149 - 4155

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被引用次数: 14

摘要

A practical and scaleable synthesis of the γ-secretase inhibitor 1 is reported. The inhibitor consists of a central trisubstituted cyclohexane core with appended propionic acid, 2, 5- difluorophenyl, and 4-chlorophenylsulfonyl moieties. Two alternative synthetic strategies, proceeding by way of a common disubstituted cyclohexanone derivative 5, were studied. In the preferred route, conjugate reduction of acrylonitrile derivative 4 with L-Selectride ...

4-氯苯硫酚结构式

2,5-二氟溴苄结构式

2,5-二氟溴苄

~99%

2-[[(4-氯苯基)硫代]甲基]-1,4-二氟苯结构式

2-[[(4-氯苯基)硫代]甲...

{cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexy l}acetonitrile结构式

{cis-4-[(4-Chlo...

~94%

2-((1s,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)acetaldehyde结构式

2-((1s,4s)-4-(4...

2-[[(4-氯苯基)硫代]甲基]-1,4-二氟苯结构式

2-[[(4-氯苯基)硫代]甲...

~%

2-((1s,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)acetaldehyde结构式

2-((1s,4s)-4-(4...

4-氯苯硫酚结构式

~%

2-((1s,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)acetaldehyde结构式

2-((1s,4s)-4-(4...

2,5-二氟溴苄结构式

2,5-二氟溴苄

~%

2-((1s,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)acetaldehyde结构式

2-((1s,4s)-4-(4...

2-((4-氯苯基磺酰基)甲基)-1,4-二氟苯结构式

2-((4-氯苯基磺酰基)甲基...

~%

2-((1s,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)acetaldehyde结构式

2-((1s,4s)-4-(4...

4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己酮结构式

4-[(4-氯苯基)磺酰基]-...

~%

2-((1s,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)acetaldehyde结构式

2-((1s,4s)-4-(4...

2-(4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexylidene)acetonitrile结构式

2-(4-(4-chlorop...

~%

2-((1s,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)acetaldehyde结构式

2-((1s,4s)-4-(4...

2-{1-[(4-Chlorophenyl)sulfonyl]vinyl}-1,4-difluorobenzene结构式

2-{1-[(4-Chloro...

~%

2-((1s,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)acetaldehyde结构式

2-((1s,4s)-4-(4...

2-(4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexylidene)acetonitrile结构式

2-(4-(4-chlorop...

~95%

{cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexy l}acetonitrile结构式

{cis-4-[(4-Chlo...

2-[[(4-氯苯基)硫代]甲基]-1,4-二氟苯结构式

2-[[(4-氯苯基)硫代]甲...

~%

{cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexy l}acetonitrile结构式

{cis-4-[(4-Chlo...

4-氯苯硫酚结构式

~%

{cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexy l}acetonitrile结构式

{cis-4-[(4-Chlo...

2,5-二氟溴苄结构式

2,5-二氟溴苄

~%

{cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexy l}acetonitrile结构式

{cis-4-[(4-Chlo...

2-((4-氯苯基磺酰基)甲基)-1,4-二氟苯结构式

2-((4-氯苯基磺酰基)甲基...

~%

{cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexy l}acetonitrile结构式

{cis-4-[(4-Chlo...

4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己酮结构式

4-[(4-氯苯基)磺酰基]-...

~%

{cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexy l}acetonitrile结构式

{cis-4-[(4-Chlo...

2-{1-[(4-Chlorophenyl)sulfonyl]vinyl}-1,4-difluorobenzene结构式

2-{1-[(4-Chloro...

~%

{cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexy l}acetonitrile结构式

{cis-4-[(4-Chlo...

4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己酮结构式

4-[(4-氯苯基)磺酰基]-...

氰甲基磷酸二乙酯结构式

氰甲基磷酸二乙酯

~97%

2-(4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexylidene)acetonitrile结构式

2-(4-(4-chlorop...

2-[[(4-氯苯基)硫代]甲基]-1,4-二氟苯结构式

2-[[(4-氯苯基)硫代]甲...

~%

2-(4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexylidene)acetonitrile结构式

2-(4-(4-chlorop...

4-氯苯硫酚结构式

~%

2-(4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexylidene)acetonitrile结构式

2-(4-(4-chlorop...

2,5-二氟溴苄结构式

2,5-二氟溴苄

~%

2-(4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexylidene)acetonitrile结构式

2-(4-(4-chlorop...

2-((4-氯苯基磺酰基)甲基)-1,4-二氟苯结构式

2-((4-氯苯基磺酰基)甲基...

~%

2-(4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexylidene)acetonitrile结构式

2-(4-(4-chlorop...

2-{1-[(4-Chlorophenyl)sulfonyl]vinyl}-1,4-difluorobenzene结构式

2-{1-[(4-Chloro...

~%

2-(4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexylidene)acetonitrile结构式

2-(4-(4-chlorop...

2-((4-氯苯基磺酰基)甲基)-1,4-二氟苯结构式

2-((4-氯苯基磺酰基)甲基...

四甲基甲烷二胺结构式

四甲基甲烷二胺

~92%

2-{1-[(4-Chlorophenyl)sulfonyl]vinyl}-1,4-difluorobenzene结构式

2-{1-[(4-Chloro...

2-[[(4-氯苯基)硫代]甲基]-1,4-二氟苯结构式

2-[[(4-氯苯基)硫代]甲...

~%

2-{1-[(4-Chlorophenyl)sulfonyl]vinyl}-1,4-difluorobenzene结构式

2-{1-[(4-Chloro...

4-氯苯硫酚结构式

~%

2-{1-[(4-Chlorophenyl)sulfonyl]vinyl}-1,4-difluorobenzene结构式

2-{1-[(4-Chloro...

2,5-二氟溴苄结构式

2,5-二氟溴苄

~%

2-{1-[(4-Chlorophenyl)sulfonyl]vinyl}-1,4-difluorobenzene结构式

2-{1-[(4-Chloro...

2,5-二氟溴苄结构式

2,5-二氟溴苄

~%

2-((4-氯苯基磺酰基)甲基)-1,4-二氟苯结构式

2-((4-氯苯基磺酰基)甲基...

4-氯苯硫酚结构式

~%

2-((4-氯苯基磺酰基)甲基)-1,4-二氟苯结构式

2-((4-氯苯基磺酰基)甲基...

2-[[(4-氯苯基)硫代]甲基]-1,4-二氟苯结构式

2-[[(4-氯苯基)硫代]甲...

~%

4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己酮结构式

4-[(4-氯苯基)磺酰基]-...

2,5-二氟溴苄结构式

2,5-二氟溴苄

~%

4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己酮结构式

4-[(4-氯苯基)磺酰基]-...

4-氯苯硫酚结构式

~%

4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己酮结构式

4-[(4-氯苯基)磺酰基]-...

2-((4-氯苯基磺酰基)甲基)-1,4-二氟苯结构式

2-((4-氯苯基磺酰基)甲基...

~%

4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己酮结构式

4-[(4-氯苯基)磺酰基]-...

2-{1-[(4-Chlorophenyl)sulfonyl]vinyl}-1,4-difluorobenzene结构式

2-{1-[(4-Chloro...

~%

4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己酮结构式

4-[(4-氯苯基)磺酰基]-...