384338-20-9Relevant articles and documents
Short enantioselective total synthesis of (+)-tofacitinib
Mane, Kishor D.,Kamble, Rohit B.,Suryavanshi, Gurunath
, (2021/02/20)
An enantioselective total synthesis of Tofacitinib (CP-690,550), a Janus tyrosine kinase (JAK3) specific inhibitor has been achieved from the readily available 4-piperidone. Proline catalysed hydroxylation is the key step for the synthesis of enantiopure 1-benzyl-4-methylpiperidin-3-ol.
Method for preparing lactam compound
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Paragraph 0163-0168, (2020/11/09)
The invention relates to a preparation method of a lactam compound, and belongs to the field of medicinal chemistry. The preparation method comprises the following steps: carrying out an asymmetric hydrogenation reaction on raw materials under the action of a ruthenium catalyst and a hydrogen donor reagent, and carrying out a post treatment to obtain the target compound. The product obtained by the method is high in ee value, the method is simple and convenient, and the target compound can be easily, conveniently and efficiently obtained.
A supporting france for cloth as the starting material of the preparation method (by machine translation)
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Paragraph 0007; 0025; 0031, (2017/12/06)
The invention discloses a method for supporting france for cloth starting material N - ((3 R, 4 R) - 4 - methyl - 1 - benzyl - 3 - piperidinyl) - N - methyl - 7 - paratoluene sulfonyl - 7 H - pyrrolo [2, 3 - D] pyrimidine - 4 - amine (I) synthetic method, specific steps are as follows: to 4 - methyl pyridine as the starting material, with the benzyl chloride undergo nucleophilic substitution by the 4 - methyl - 1 - phenylmethyl - pyridine hydrochloride, under the action of the sodium borohydride reduction reaction, borohydrite - oxidation reaction, hydroxy oxidation, the introduction of the reductive amination of the stereo selectivity of the two chiral center, through a readily available and inexpensive chiral acid (L - DTTA) splitting, to obtain optically pure intermediates (3 R, 4 R) - (1 - benzyl - 4 - methyl - piperidin - 3 - yl) - methylamine, and finally with the 4 - chloro pyrrolo pyrimidine condensation is obtained. The whole method raw materials are easy, simple operation, after treatment is easy, and the cost is low. (by machine translation)