Method for preparing chiral 1, 2, 3, 4-tetrahydro-1-naphthoic acid

A naphthoic acid and chiral technology, which is applied in the field of preparation of chiral 1, can solve the problems of serious environmental pollution of chromium trioxide oxidant, and achieve the effects of easy separation and purification, mild conditions and mild reaction conditions
CN101591241BActive Publication Date: 2013-01-02国药集团工业有限公司 +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
国药集团工业有限公司
Publication Date
2013-01-02

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Abstract

The invention provides a method for preparing chiral 1, 2, 3, 4-tetrahydro-1-naphthoic acid. The method takes the chiral 1, 2, 3, 4-tetrahydro-1-napthyl methanol as the raw material, and the raw material is oxidized under the existence of oxidant to obtain the carboxylic acid with a corresponding configuration. The method is simple in circuit, simple and convenient to operate, high in yield, and suitable for industrial production.
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Description

technical field

[0001] The invention relates to the field of medicinal chemistry, in particular to a method for preparing chiral 1,2,3,4-tetrahydro-1-naphthoic acid. Background technique

[0002] Palonosetron hydrochloride (Palonosetron), trade name Aloxi (Aloxi), belongs to 5-HT 3 Receptor antagonists for the prevention of acute and delayed emesis caused by moderately or highly emetogenic chemotherapy regimens. Developed by Swiss company Helsinn, it was first launched in the United States in September 2003. In 2006, the global sales of the drug reached 250 million US dollars. The drug is characterized by low dose, long action time, and little toxic and side effects, and occupies an important position in antiemetic drugs.

[0003] Document US5510486 reports that the key intermediate of palonosetron hydrochloride (S)-1,2,3,4-tetrahydro-1-naphthoic acid is synthesized by a resolution method, using quinine as a resolution agent to resolve and eliminate Rotated 1,2,3,4-tetr...

Claims

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