THERMODYNAMICALLY STABLE CRYSTAL FORM OF 4''-DEOXY-4''-EPI-METHYLAMINO AVERMECTIN B1A/B1B BENZOIC ACID SALT AND PROCESS FOR PREPARING THE SAME

Title:

THERMODYNAMICALLY STABLE CRYSTAL FORM OF 4''-DEOXY-4''-EPI-METHYLAMINO AVERMECTIN B1A/B1B BENZOIC ACID SALT AND PROCESS FOR PREPARING THE SAME

Document Type and Number:

Japanese Patent JP2011207899

Kind Code:

A

Abstract:

To provide the most stable crystalline form of 4"-deoxy-4"-epi-methlamino avermectin B1a/B1b benzoic acid salt from four crystalline forms of that salt which is an agricultural insecticide, and to provide a process for preparing the same.

The most thermodynamically stable crystalline form of the benzoic acid salt of 4''-deoxy-4''-epi-methylamino avermectin B1a/B1b as the hemihydrate is obtained by crystallization from organic solvents containing a controlled amount of water. The crystalline form salt is extremely important in that it provides bulk material with crystal homogeneity which is not going to transform to another crystal form during storage.

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Inventors:

CVETOVICH RAYMOND
DEMCHAK RICHARD
MCCAULEY JAMES A
VARSALONA RICHARD J

Application Number:

JP2011117141A

Publication Date:

October 20, 2011

Filing Date:

May 25, 2011

Export Citation:

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Assignee:

MERCK SHARP & DOHME

International Classes:

C07H17/08; A01N43/22; A01N43/90; A01N63/02; A01P7/04; C07D493/22; C07H17/04; C07H19/01

Domestic Patent References:

JPH0320270A	1991-01-29
JPS57212200A	1982-12-27
JPS6236384A	1987-02-17
JPH0543590A	1993-02-23
JPH0446192A	1992-02-17
JPH03240794A	1991-10-28
JPH02134393A	1990-05-23
JPH0578352A	1993-03-30

Foreign References:

CA2045864A1	1991-12-29
WO1992020683A1	1992-11-26

Other References:

JPN6011052096; 新・薬剤学総論（改訂第３版） , 19870410, ｐ．１１１，２５６-２５７，３２７, 株式会社南江堂
JPN6011052099; 調剤学-基礎と応用- , 19770920, ｐ．１４２-１４５, 株式会社南山堂

Attorney, Agent or Firm:

Yoshio Kawaguchi
Katsuma Osaki

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