Efficient synthesis of a key intermediate of DV-7751 via optical resolution or microbial reduction.

Abstract:

:Two efficient and practical methods of synthesis of the C-10 substituent of DV-7751 (1), a novel quinolone carboxylic acid, were established. The first method utilizes an optical resolution of racemic 8-amino-6-benzyl-6-azaspiro[3.4]octane (13), while the second employs an enantioselective microbial reduction of 6-benzyl-5,8-dioxo-6-azaspiro[3.4]octane (8b). The enantiomeric excess of (S)-8-amino-6-benzyl-6-azaspiro[3.4]octane (11) with each method of synthesis is greater than 96%.

authors

Miyadera A,Satoh K,Imura A

doi

10.1248/cpb.48.563

subject

Has Abstract

pub_date

2000-04-01 00:00:00

pages

563-5

issue

4

eissn

0009-2363

issn

1347-5223

journal_volume

48

pub_type

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