A kind of preparation method of 2-(4-phenoxyphenyl)-6-(n-substituted oxycarbonyl piperidine-4-) base nicotinamide

A technology of phenoxyphenyl and base carbonyl piperidine is applied in the field of preparation of 2--6-yl nicotinamide, and achieves the effects of low cost, easy operation of technological process, and cheap and readily available raw materials
CN113563305BActive Publication Date: 2022-07-01XINFA PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
XINFA PHARMA
Publication Date
2022-07-01

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Abstract

The invention provides a preparation method of 2-(4-phenoxyphenyl)-6-(N-substituted oxycarbonyl piperidine-4-) base nicotinamide, the method utilizes 3-nitropropionaldehyde and 3-nitropropionaldehyde -(4-phenoxyphenyl)-3-oxo-propionamide obtains 2-(4-phenoxybenzoyl)-5-nitro-n-pentane through the first condensation reaction under the action of an acid catalyst -2-enamide, then under the action of alkali and N-substituted oxycarbonyl piperidine-4-ketone through the second condensation reaction to obtain 2-(4-phenoxybenzoyl)-5-nitro- The reaction of 5-(N-substituted oxycarbonyl-4-hydroxy-4-yl) piperidinyl n-pent-2-enamide, adding ammonium salt, catalyst, under temperature-programmed conditions, through reduction-cyclization reaction and Isomerization reaction to obtain 2-(4-phenoxyphenyl)-6-(N-substituted oxycarbonyl piperidine-4-) base nicotinamide. The raw materials used in the invention are cheap and easy to obtain, the technological process is easy to operate, the target product has low cost, high yield and high purity, and is suitable for industrial production.
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Description

technical field

[0001] The invention relates to a preparation method of 2-(4-phenoxyphenyl)-6-(N-substituted oxycarbonylpiperidin-4-)yl nicotinamide, and belongs to the technical field of medicine and chemical industry. Background technique

[0002] 2-(4-Phenoxyphenyl)-6-(N-substituted oxycarbonylpiperidin-4-)ylnicotinamide (I) is an important pyridine derivative that can be used to prepare Orelabrutinib ). Orelabrutinib, CAS No. [1655504-04-3], is a specific and selective BTK inhibitor developed by China Nuocheng Jianhua, China National Medical Products Administration (NMPA) has accepted Orelabrutinib (ICP-022) New drug listing for the treatment of relapsed / refractory chronic lymphocytic leukemia (CLL) and the treatment of relapsed or refractory chronic lymphocytic leukemia / small lymphocytic lymphoma (CLL / SLL), application for the treatment of tumors and For autoimmune diseases, the overall efficacy of orelabrutinib is better than that of ibrutinib, and the safety factor ...

Claims

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