IP Library › Granted Patent US 9,938,228
Granted Patent B2
US 9,938,228 · App. 15/509,504 · Granted Apr 10, 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
C07C69/608C07C45/54C07C45/673C07C59/205C07C67/347C07C69/716C07C69/757
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Quick Facts
Patent No.
US 9,938,228
App. No.
15/509,504
Granted
Apr 10, 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[2.5]octane-5,7-dione having the formula

said method

comprising:

cyclization of cyclopropylidene carboxylic acid alkyl ester having the formula

with dialkyl 1,3-acetonedicarboxylate having the formula

to form 5,7-dioxo-spiro[2.5]octane-4,6-dicarboxylic acid dialkyl ester having the formula

wherein each R may be independently C1-C6 alkyl,

and

ester hydrolysis and decarboxylation of 5,7-dioxo-spiro[2.5]octane-4,6-dicarboxylic acid to form spiro[2.5]octane-5,7-dione,

wherein each R may be independently C1-C6 alkyl.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 8, 2017
From: JIN, XIANGLE; DONG, WEITONG; FU, YAN; LU, JUN; XIE, LE; XU, WEI; YNAG, JINSONG; ZHU, QIAN
To: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Reel/Frame 042273/0673 →
Priority Claims (1)
WO PCT/CN2014/086143 · Sep 9, 2014 · international
Continuity (1)
Related Publication 20170247315A1 · Aug 31, 2017