PRODUCTION OF 3,7-DISUBSTITUTED INDOLE DERIVATIVE AND OPTICALLY ACTIVE ISOMER THEREOF

Title:

PRODUCTION OF 3,7-DISUBSTITUTED INDOLE DERIVATIVE AND OPTICALLY ACTIVE ISOMER THEREOF

Document Type and Number:

Japanese Patent JP2000319256

Kind Code:

A

Abstract:

To obtain an optically active (aminoalkyl)-substituted indole derivative, useful as the intermediate for a compound having a β3 adrenergic acceptor stimulant action, by methathesis of the salt obtained by reacting a specific derivative with a specific acid.

This optically active 3-(2'-aminoalkyl)-7-substituted indole derivative, shown by formula III, is obtained by reacting (A) a (±)-3-(2'-aminoalkyl)-7- substituted indole derivative shown by formula I [R1 is a lower alkyl or aralkyl; and R2 is a (cyclic) lower alkyl] with (B) 0.5 to 1 equivalent of an optically active organic salt shown by the formula A*H in the presence of (C) a solvent to form the salt (D) of the components A and B, shown by formula II [(n) is 0.5 to 1], and then by methathesis of the isolated salt (D). The compounds useful as the component B include a monobasic acid of L-mandelic acid or the like, and dibasic acid of L-ditoluoyl tartrate, the latter being more preferable.

Inventors:

IKENAKA MASAYA
FUJIMA YOSHITO
KATO SHIROU
HARADA HIROSHI
FUJII AKIHITO

Application Number:

JP12858699A

Publication Date:

November 21, 2000

Filing Date:

May 10, 1999

Export Citation:

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Assignee:

DAINIPPON PHARMACEUTICAL CO
NAGASE & CO LTD

International Classes:

C07D209/14; B01J25/00; B01J25/02; (IPC1-7): C07D209/14; B01J25/00; B01J25/02

Attorney, Agent or Firm:

Aoyama Ryo (1 person outside)

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