Synthesis utilizing insoluble polymers: new reactions and small molecules

被引:14
作者
Baxter, AD [1 ]
机构
[1] Oxford Divers, Abingdon OX14 4RX, Oxon, England
关键词
D O I
10.1016/S1367-5931(97)80112-3
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
It can be argued that solid-phase organic chemistry is the preferred method of preparing screening libraries for lead compound discovery and lead optimization within the pharmaceutical industry, Solid-phase peptide chemistry is the most reliable and general of the synthetic methods available today; however, the purities of products are inadequate for the needs of the current market and the screening departments of pharmaceutical companies. Recent synthetic advances in solid-phase organic chemistry have started to increase the range of chemistry that can be used to prepare 'drug-like' small molecules in library format.
引用
收藏
页码:79 / 85
页数:7
相关论文
共 49 条
[31]   THE SOLID-PHASE SYNTHESIS OF DIHYDROISOQUINOLINES AND TETRAHYDROISOQUINOLINES [J].
MEUTERMANS, WDF ;
ALEWOOD, PF .
TETRAHEDRON LETTERS, 1995, 36 (42) :7709-7712
[32]   Pictet-Spengler reaction on solid support: Synthesis of 1,2,3,4-tetrahydro-beta-carboline libraries [J].
Mohan, R ;
Chou, YL ;
Morrissey, MM .
TETRAHEDRON LETTERS, 1996, 37 (23) :3963-3966
[33]   A novel linker strategy for solid-phase synthesis [J].
Morphy, JR ;
Rankovic, Z ;
Rees, DC .
TETRAHEDRON LETTERS, 1996, 37 (18) :3209-3212
[34]   COMBINATORIAL ORGANIC-SYNTHESIS OF HIGHLY FUNCTIONALIZED PYRROLIDINES - IDENTIFICATION OF A POTENT ANGIOTENSIN-CONVERTING ENZYME-INHIBITOR FROM A MERCAPTOACYL PROLINE LIBRARY [J].
MURPHY, MM ;
SCHULLEK, JR ;
GORDON, EM ;
GALLOP, MA .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1995, 117 (26) :7029-7030
[35]   Tamoxifen-induced proto-oncogene expression persists in uterine endometrial epithelium [J].
Nephew, KP ;
Polek, TC ;
Khan, SA .
ENDOCRINOLOGY, 1996, 137 (01) :219-224
[36]   The use of anion exchange resins for the synthesis of combinatorial libraries containing aryl and heteroaryl ethers [J].
Parlow, JJ .
TETRAHEDRON LETTERS, 1996, 37 (30) :5257-5260
[37]   The design and synthesis of substituted biphenyl libraries [J].
Pavia, MR ;
Cohen, MP ;
Dilley, GJ ;
Dubuc, GR ;
Durgin, TL ;
Forman, FW ;
Hediger, ME ;
Milot, G ;
Powers, TS ;
Sucholeiki, I ;
Zhou, SL ;
Hangauer, DG .
BIOORGANIC & MEDICINAL CHEMISTRY, 1996, 4 (05) :659-666
[38]   A SILICON-BASED LINKER FOR TRACELESS SOLID-PHASE SYNTHESIS [J].
PLUNKETT, MJ ;
ELLMAN, JA .
JOURNAL OF ORGANIC CHEMISTRY, 1995, 60 (19) :6006-6007
[39]   SOLID-PHASE SYNTHESIS OF ARYL ETHERS VIA THE MITSUNOBU REACTION [J].
RANO, TA ;
CHAPMAN, KT .
TETRAHEDRON LETTERS, 1995, 36 (22) :3789-3792
[40]  
Rolfing K, 1996, SYNLETT, P1036