344419-25-6Relevant academic research and scientific papers
Synthetic method for compound
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Paragraph 0051-0053; 0059-0060; 0062-0063, (2019/12/25)
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.
A method for synthesis of piperidine derivatives (by machine translation)
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, (2018/10/19)
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)
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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, (2016/10/09)
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.
A novel asymmetric synthesis of cis-(3R,4R)-N-(tert -butoxycarbonyl)-4- methyl-3-(methylamino)piperidine
Hao, Bao-Yu,Liu, Jin-Qiang,Zhang, Wei-Han,Chen, Xin-Zhi
, p. 1208 - 1212 (2011/05/30)
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
