Solid phase synthesis of spiroindoline

被引:37
作者
Cheng, Y
Chapman, KT
机构
[1] Automated Sythesis Group, Dept. of Molec. Des. and Diversity, Merck Research Laboratories, Rahway
关键词
COMBINATORIAL TECHNOLOGIES; DRUG DISCOVERY;
D O I
10.1016/S0040-4039(97)00139-1
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A method for solid phase synthesis of spiroindolines using the Fischer indole reaction is described. Various arylhydrazines react cleanly with polymer bound piperidine-4-carboxaldehyde in TFA/CH2Cl2. The products are isolated in good yields and high purity. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码:1497 / 1500
页数:4
相关论文
共 7 条
[1]   APPLICATIONS OF COMBINATORIAL TECHNOLOGIES TO DRUG DISCOVERY .1. BACKGROUND AND PEPTIDE COMBINATORIAL LIBRARIES [J].
GALLOP, MA ;
BARRETT, RW ;
DOWER, WJ ;
FODOR, SPA ;
GORDON, EM .
JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (09) :1233-1251
[2]   APPLICATIONS OF COMBINATORIAL TECHNOLOGIES TO DRUG DISCOVERY .2. COMBINATORIAL ORGANIC-SYNTHESIS, LIBRARY SCREENING STRATEGIES, AND FUTURE-DIRECTIONS [J].
GORDON, EM ;
BARRETT, RW ;
DOWER, WJ ;
FODOR, SPA ;
GALLOP, MA .
JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (10) :1385-1401
[3]  
HUTCHINS SM, 1996, TETRAHEDRON LETT, V32, P7571
[4]  
MALIGRES PE, 1997, IN PRESS TETRAHEDRON
[5]   DESIGN AND BIOLOGICAL-ACTIVITIES OF L-163,191 (MK-0677) - A POTENT, ORALLY-ACTIVE GROWTH-HORMONE SECRETAGOGUE [J].
PATCHETT, AA ;
NARGUND, RP ;
TATA, JR ;
CHEN, MH ;
BARAKAT, KJ ;
JOHNSTON, DBR ;
CHENG, K ;
CHAN, WWS ;
BUTLER, B ;
HICKEY, G ;
JACKS, T ;
SCHLEIM, K ;
PONG, SS ;
CHAUNG, LYP ;
CHEN, HY ;
FRAZIER, E ;
LEUNG, KH ;
CHIU, SHL ;
SMITH, RG .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1995, 92 (15) :7001-7005
[6]   RECENT STUDIES ON FISCHER INDOLE SYNTHESIS [J].
ROBINSON, B .
CHEMICAL REVIEWS, 1969, 69 (02) :227-+
[7]   Synthesis and applications of small molecule libraries [J].
Thompson, LA ;
Ellman, JA .
CHEMICAL REVIEWS, 1996, 96 (01) :555-600