1187595-85-2Relevant articles and documents
PYRAZOLYL PYRROLO[2,3-B]PYRMIDINE-5-CARBOXYLATE ANALOGS AND METHODS OF MAKING THE SAME
-
Paragraph 0296-0297, (2019/05/18)
The present invention relates to new pyrrolopyridine compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of JAK1 and JAK3 kinase activity in a human or animal subject are also provided for the treatment diseases such as pruritus, alopecia, androgenetic alopecia, alopecia areata, vitiligo and psoriasis.
Preparation method for synthesizing key intermediate 1 of Baricitinib
-
Paragraph 0050; 0051; 0058, (2018/04/03)
The invention relates to a preparation method for synthesizing a key intermediate 1 of Baricitinib. The preparation method comprises the following steps: generating ring closing reaction by virtue of1,3-dibromo-2,2-dimethoxypropane (SM) and ethyl sulfonamide (SM2) under an alkaline condition, and carrying out acetal deprotection under an acidic condition, so as to obtain an intermediate B; and generating witting reaction by virtue of the obtained intermediate B and diethyl cyanomethylphosphonate under the alkaline condition, so as to obtain the key intermediate 1. According to the preparationmethod, the ring closing reaction is generated by virtue of the commercial materials SM and ethyl sulfonamide under the alkaline condition, acetal deprotection is carried out under the acidic condition so as to obtain intermediate B, and witting reaction is carried out so as to obtain the key intermediate 1; the key intermediate 1 can be actually obtained only through two synthetic steps; and compared with the prior art, the preparation method has the advantages that the synthetic route is greatly shortened, the hydrogenation is avoided, and the production cost of the key intermediate 1 is lowered.
Novel synthetic method for baricitinib and intermediate thereof
-
Paragraph 0056-0058, (2017/08/18)
The invention discloses a novel intermediate compound 5 of baricitinib. The compound 5 has stable properties, which is favorable for separation and purification. The invention also discloses a preparation method for the compound 5 and two schemes for preparing baricitinib from the baricitinib. The two schemes are simple in operation, shortened in reaction steps, high in yield and product purity and suitable for enlarged production. The compound 5 has a structural formula as defined in the specification. In the formula, X represents halogen, e.g., chlorine, bromine or iodine.