An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals

被引：487

作者：

Baumann, Marcus ^{[1
]}

Baxendale, Ian R. ^{[1
]}

Ley, Steven V. ^{[1
]}

Nikbin, Nikzad ^{[1
]}

机构：

[1] Univ Cambridge, Dept Chem, Innovat Technol Ctr, Cambridge CB2 1EW, England

来源：

BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY | 2011年 / 7卷

基金：

英国工程与自然科学研究理事会;

关键词：

five-membered rings; heterocycles; medicinal chemistry; pharmaceuticals; synthesis; 5-SUBSTITUTED INDOLE-DERIVATIVES; II RECEPTOR ANTAGONISTS; ONE-POT SYNTHESIS; CYCLOOXYGENASE-2; INHIBITORS; BIOLOGICAL EVALUATION; PRACTICAL SYNTHESIS; EFFICIENT SYNTHESIS; COUPLING REACTION; 5-HT1D RECEPTOR; IV INHIBITOR;

D O I：

10.3762/bjoc.7.57

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

This review presents a comprehensive overview on selected synthetic routes towards commercial drug compounds as published in both journal and patent literature. Owing to the vast number of potential structures, we have concentrated only on those drugs containing five-membered heterocycles and focused principally on the assembly of the heterocyclic core. In order to target the most representative chemical entities the examples discussed have been selected from the top 200 best selling drugs of recent years.

引用

页码：442 / 495

页数：54

共 142 条

[1]

AIKINS JA, 1996, Patent No. 9640691

[2]

ALBINSON FD, 1992, Patent No. 5103020

[3]

ASHCROFT CP, 2001, Patent No. 1088817

[4]

ASHCROFT CP, 2005, Patent No. 2005103035

[5]

Baker R., 1994, US patent, Patent No. [5298520, 5,298,520]

[6] Synthesis of [1,2,4]triazolo[4,3-α,]piperazines via highly reactive chloromethyloxadiazoles [J].

Balsells, J ;

DiMichele, L ;

Liu, JC ;

Kubryk, M ;

Hansen, K ;

Armstrong, JD .

ORGANIC LETTERS, 2005, 7 (06) :1039-1042

[7] Pharmaceutical strategy and innovation: An academics perspective [J].

Baxendale, Ian R. ;

Hayward, John J. ;

Ley, Steven V. ;

Tranmer, Geoffrey K. .

CHEMMEDCHEM, 2007, 2 (06) :768-788

[8]

BERGLUND RA, 1996, Patent No. 5491243

[9]

Bischler A., 1892, CHEM BER-RECL, V25, P2860, DOI [10.1002/cber.189202502123, DOI 10.1002/CBER.189202502123]

[10] AN ENANTIOSELECTIVE SYNTHESIS OF THE TOPICALLY-ACTIVE CARBONIC-ANHYDRASE INHIBITOR MK-0507 - 5,6-DIHYDRO-(S)-4-(ETHYLAMINO)-(S)-6-METHYL-4H-THIENO[2,3-B]THIOPYRAN-2-SULFONAMIDE 7,7-DIOXIDE HYDROCHLORIDE [J].

BLACKLOCK, TJ ;

SOHAR, P ;

BUTCHER, JW ;

LAMANEC, T ;

GRABOWSKI, EJJ .

JOURNAL OF ORGANIC CHEMISTRY, 1993, 58 (07) :1672-1679

← 1 2 3 4 5 6 7 8 9 10 →