- Synthetic method for compound
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The invention provides a synthetic method for a compound having a structural formula represented by a formula (V) shown in the specification. The method comprises the following steps: 1) performing hydrodebenzylation on a compound having a structural formula represented by a formula (I) shown in the specification to obtain a compound having a structural formula represented by a formula (II) shownin the specification; 2) allowing a compound having a structural formula represented by a formula (III) to be in contact with the compound having the structural formula represented by the formula (II)to obtain a compound having a structural formula represented by a formula (IV) shown in the specification; and 3) allowing the compound having the structural formula represented by the formula (IV) to be in contact with an acid solution to remove t-butoxycarbonyl protection, so as to obtain the compound having the structural formula represented by the formula (V). The synthetic method provided bythe invention has the advantages of a short synthetic route, a simple process, easy availability of the raw materials, simple post-treatment, good quality and a high yield, and is suitable for industrial production of tasocitinib and an intermediate of the tasocitinib.
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Paragraph 0051-0053; 0059-0060; 0062-0063
(2019/12/25)
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- A method for synthesis of piperidine derivatives (by machine translation)
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The invention discloses a method for synthesis of piperidine derivatives. The piperidine derivatives of the formula (I) of the tartrate: Wherein R1 Is an amino protecting group, R2 Is phenyl or alkyl substituted phenyl, R3 Is C1 - C6 alkyl; by the piperidine derivative having the structural formula (II) with a compound L - tartaric acid reaction, then the obtained through separation, In the having piperidine 3 bit reference into the S on amino-substituted radical, can significantly improve the for tartaric acid from L - In the separate The effect of the. The method can be used for the synthesis of pharmaceutical Tofacitinib, in order to improve the yield of drug Tofacitinib. (by machine translation)
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- The protection of the nitrogen of (3R, 4R) -3 - methylamino -4 - methyl piperidine asymmetric synthesis method, relevant intermediate and a method for preparing raw materials thereof
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The invention relates to a preparation method of nitrogen protected (3R,4R)-3-methylamino-4-methylpiperidine (I). The method comprises the following steps: carrying out a reductive amination reaction on a compound of formula (III) and (R)-1-phenylethylamine to obtain a compound of formula (II), removing chiral prosthetic groups from the compound of formula (II), and adding a methyl group to the amino group of the compound of formula (II) in order to obtain nitrogen protected (3R,4R)-3-methylamino-4-methylpiperidine (I), wherein R in each of the formula (I), the formula (II) and the formula (III) is an amino protection group or hydrogen, and the amino protection group can be C1-4 alkoxycarbonyl, benzyloxycarbonyl or benzyl groups which can be removed through hydrolysis or hydrogenation. The asymmetric synthesis method of nitrogen protected (3R,4R)-3-methylamino-4-methylpiperidine (I) has the advantages of reasonable technology, concise route, obtaining of the required product in a high ee value manner by constructing two chiral centers through chiral induced one-step reductive amination, cheap raw materials, and no waste isomer emission, and is suitable for large-scale industrialized production.
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- A novel asymmetric synthesis of cis-(3R,4R)-N-(tert -butoxycarbonyl)-4- methyl-3-(methylamino)piperidine
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cis-(3R,4R)-N-(tert-Butoxycarbonyl)-4-methyl-3-(methylamino)piperidine, a key intermediate for the synthesis of CP-690550 (a potent protein kinase inhibitor), is prepared via an asymmetric approach starting from ethyl 1-benzyl-3-oxopiperidine-4-carboxylat
- Hao, Bao-Yu,Liu, Jin-Qiang,Zhang, Wei-Han,Chen, Xin-Zhi
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p. 1208 - 1212
(2011/05/30)
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