The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 7795472 B1

PDF
Full Text
Expired
Date of Patent:
Sep. 14, 2010

Filed:

Oct. 07, 2005
Applicants:

Takeshi Tsubuki, Oyama, JP;

Kenichi Kobayashi, Koshigaya, JP;

Hidetaka Komatsu, Shimotsuga-gun, JP;

Inventors:

Takeshi Tsubuki, Oyama, JP;

Kenichi Kobayashi, Koshigaya, JP;

Hidetaka Komatsu, Shimotsuga-gun, JP;

Assignee:
Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07C 215/00 (2006.01); C07C 321/00 (2006.01); C07C 323/00 (2006.01); C07C 381/00 (2006.01); C07C 209/00 (2006.01); C07C 213/00 (2006.01);
U.S. Cl.
CPC ...
Abstract

A process for the industrial production of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride (Compound I), an effective immunosuppressant. The process for producing 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride or a hydrate thereof includes the steps of reacting 4-(3-benzyloxyphenylthio)-2-chlorobenzaldehyde with ethyl diethylphosphonoacetate in a solvent in the presence of a base to form ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate; reducing the resulting ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate, followed by mesylation, iodination and nitration, to form 1-benzyloxy-3-[3-chloro-4-(3-nitropropyl)phenylthio]benzene; forming 2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-2-nitro-1,3-propanediol using a formaldehyde solution; and reducing the resulting 2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-2-nitro-1,3-propanediol to form the desired product.


Find Patent Forward Citations

Tsubuki, Takeshi. (2010). Process for producing 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride and hydrates thereof, and intermediates in the production thereof (U.S. Patent No. 7795472). U.S. Patent and Trademark Office. https://idiyas.com/patent/badge/7795472

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