IP Library › Granted Patent US 10,131,618
Granted Patent B2
US 10,131,618 · App. 15/904,464 · Granted Nov 20, 2018

Process for the preparation of spiro[2.5]octane-5,7-dione and spiro[3.5]nonane-6,8-dione

Inventors: Xiangle Jin (Shanghai, CN); Weitong Dong (Shanghai, CN); Yan Fu (Shanghai, CN); Jun Lu (Shanghai, CN); Le Xie (Shanghai, CN); Wei Xu (Shanghai, CN); Jinsong Yang (Shanghai, CN); Qian Zhu (Shanghai, CN)
Assignee: Boehringer Ingelheim International GmbH
C07C69/608C07C45/54C07C45/673C07C59/205C07C67/347C07C69/716C07C69/757C07C2601/02C07C2601/04C07C2602/50
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Quick Facts
Patent No.
US 10,131,618
App. No.
15/904,464
Granted
Nov 20, 2018
Kind
B2
Abstract

This invention relates to methods for the synthesis of spiro[2.5]octane-5,7-dione and spiro[3.5]nonane-6,8-dione which are useful as intermediates in the manufacture of pharmaceutically active ingredients.

Claims (10)

1. A method of preparing spiro[3.5]nonane-6,8-dione having the formula

said method comprising:

cyclization of cyclobutylidene carboxylic acid alkyl ester having the formula

with dialkyl 1,3-acetonedicarboxylate having the formula

to form 6,8-dioxo-spiro[3.5]nonane-5,7-dicarboxylic acid dialkyl ester having the formula

wherein each R may be independently C1-C6 alkyl,

and

ester hydrolysis and decarboxylation of 6,8-dioxo-spiro[3.5]nonane-5,7-dicarboxylic acid dialkyl ester having the formula

to form spiro[3.5]nonane-6,8-dione,

wherein each R may be independently C1-C6 alkyl.

Priority Claims (1)
WO PCT/CN2014/086143 · Sep 9, 2014 · international
Continuity (2)
Division 15509504
Related Publication 20180179142A1 · Jun 28, 2018