Method for preparing almotriptan malate

A technology of almotriptan and malic acid, applied in the field of medicinal chemical synthesis, can solve the problems of insecurity, increased production cost, inconvenience and the like
CN102827062AInactive Publication Date: 2012-12-19YANGTZE RIVER PHARM GRP SICHUAN HAIRONG PHARM CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
YANGTZE RIVER PHARM GRP SICHUAN HAIRONG PHARM CO LTD
Publication Date
2012-12-19
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides a method for preparing almotriptan malate, which comprises that (1) 4-(1-pyrrolidinylsulforylmenthyl)phenylhydrazine and 4-chlorobutyraldehyde are reacted with each other to obtain the corresponding phenylhydrazone, and 3-[2-(dimethylamino)ethyl]-5-(1-pyrrolidinylsulforylmenthyl)-1H-benzazole (ATP-2) is formed through cyclization under the acid condition; (2) ATP-2 is methylated under the action of formaldehyde and sodium borohydride to obtain crude almotriptan alkali (ATP-3); (3) the crude almotriptan alkali (ATP-3) is respectively salified and crystallized in fumaric acid and salicylic acid ethanol solution; and (4) the refined ATP-3 and DL-malic acid are reacted with each other in carbine to obtain the almotriptan malate. The almotriptan malate with high purity can be prepared through adopting the method; and the method has a simple synthetic technology, easily obtained raw materials, high product yield and low impurity content, and can satisfy the requirement of industrial large-scale production.
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Description

technical field

[0001] The invention belongs to the field of medicinal chemical synthesis, in particular to a preparation method of almotriptan malate. Background technique

[0002] Almotriptan malate, chemical name is 3-[2-(dimethylamino)ethyl]-5-(1-pyrrolidinylsulfonylmethyl)-1H-indole malate , is a migraine treatment drug for adolescents and adults. It was first listed in Spain in September 2000, and was approved by the US FDA in May 2001 for the treatment of adult migraine.

[0003] Almotriptan malate is a brand-new chemically synthesized compound. There are not many synthetic methods reported in the literature. Almost all synthetic routes start from p-aminobenzenesulfonylpyrrole (compound II), and then obtain through different methods. Target compound:

[0004]

[0005] For example, the method described in ES2084560 is a synthetic method originally reported by the original manufacturer. The compound II is diazotized to obtain the corresponding hydrazine, and then a...

Claims

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