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Title:
COMBINED REACTION PROCESS FOR PRODUCTION OF TERTIARY AMINE COMPOUND LIBRARY BY TAKING ADVANTAGE OF SCAVENGER
Document Type and Number:
Japanese Patent JPH10120631
Kind Code:
A
Abstract:

To obtain the subject compound useful for discovering a new lead compound for developing medicines by a combined reaction in a liquid phase.

This combined reductive amination reaction process by using a scavenger comprises producing a library of a compound having a tertiary amine skeleton containing three reversible substituent groups. Each library compound is shown by formula I (R1, R2 and R3 are each a nonobstructive substituent group) and is obtained by adding an aldehyde of the formula R3CHO to a reaction region containing a liquid medium, then adding a secondary amine reagent of formula II to the reaction region, then maintaining the reaction system at a temperature for a time to enable the reductive amination of the compound of formula II, adding an amine reactive scavenger of formula III (P is an insoluble solid support; L is a bondable group; (ARS) is an amine reactive substituent group), maintaining the reaction system at a temperature for a time to react the amine reagent with the scavenger, separating the solid support scavenger and recovering the tertiary amine library compound. The reaction is carried out generally at -10°C to 60°C under normal pressure.


Inventors:
HAHN PATRIC JAMES
KALDOR STEPHEN WARREN
SIEGEL MILES GOODMAN
DRESSMAN BRUCE ANTHONY
FRITZ JAMES ERWIN
Application Number:
JP15856397A
Publication Date:
May 12, 1998
Filing Date:
June 16, 1997
Export Citation:
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Assignee:
LILLY CO ELI
International Classes:
G01N33/15; B01J19/00; B01L3/00; C07B61/00; C07C209/00; C07C211/03; C07D207/08; C07D209/42; C07D209/88; C07D211/60; C07D213/38; C07D213/50; C07D215/18; C07D241/20; C07D249/18; C07D265/30; C07D277/04; C07D295/08; C07D295/18; C07D303/02; C07D307/46; C07D307/52; C07D317/28; C07D319/12; C07D333/22; C07D333/28; C07D333/42; C07D405/12; C40B60/14; (IPC1-7): C07C211/03; C07D209/42; C07D209/88; C07D213/38; C07D213/50; C07D215/18; C07D241/20; C07D265/30; C07D277/04; C07D295/08; C07D295/18; C07D303/02; C07D307/46; C07D317/28; C07D319/12; C07D333/22; C07D333/28; C07D333/42; C07D405/12; G01N33/15
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)