1222491-53-3Relevant articles and documents
Preparation method of key intermediate of JAK3 enzyme inhibitor
-
, (2021/07/17)
The invention relates to a preparation method of a key intermediate ((3R,6S)-1-benzyl-6-methyl piperidine-3-amine) of a JAK3 enzyme inhibitor, and particularly relates to a method for preparing the required intermediate by taking 6-methyl piperidine-3-amine as an initial raw material through Boc protection, catalytic hydrogenation, benzyl protection, trifluoroacetic acid Boc de-protection, salt forming and splitting, and dissociation. The salt forming and splitting method comprises the following steps: mixing a racemic mixture containing a compound enantiomer with a structure shown in the formula with a splitting reagent with definite stereo-specificity in a solvent to form a solution, wherein the splitting agent is capable of binding at least one but not all of said enantiomers to form a precipitate containing the at least one the stereo-specific form of enantiomers; and collecting and purifying the precipitate , or collecting a solution containing other enantiomers and recrystallizing the enantiomers contained in the solution. The preparation method has the advantages of cheap and easily available raw materials, mild reaction conditions, high reaction controllability and good industrial application prospect.
PYRROLO [2,3-d] PYRIMIDINE TOSYLATE, CRYSTALLINE FORMS THEREOF, AND PREPARATION METHOD AND INTERMEDIATE THEREOF
-
, (2020/05/29)
PROBLEM TO BE SOLVED: To provide a drug molecule in a novel or purer polymorphic form. SOLUTION: In the present invention, disclosed is a novel p-toluenesulfonate of 1-((2S,5R)-5-((7H-pyrrolo [2,3-d] pyrimidin-4-yl) amino)-2-methyl piperidin-1-yl) prop-2-en-1-one and a crystalline polymorphic form 1 thereof, a pharmaceutical composition comprising the same, and their preparation and use. In the present invention, also disclosed is a novel phosphate of 1-((2S,5R)-5-((7H-pyrrolo [2,3-d] pyrimidin-4-yl) amino)-2-methyl piperidin-1-yl) prop-2-en-1-one, a pharmaceutical composition comprising the same, and their preparation and use. SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2020,JPOandINPIT
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans
Thorarensen, Atli,Dowty, Martin E.,Banker, Mary Ellen,Juba, Brian,Jussif, Jason,Lin, Tsung,Vincent, Fabien,Czerwinski, Robert M.,Casimiro-Garcia, Agustin,Unwalla, Ray,Trujillo, John I.,Liang, Sidney,Balbo, Paul,Che, Ye,Gilbert, Adam M.,Brown, Matthew F.,Hayward, Matthew,Montgomery, Justin,Leung, Louis,Yang, Xin,Soucy, Sarah,Hegen, Martin,Coe, Jotham,Langille, Jonathan,Vajdos, Felix,Chrencik, Jill,Telliez, Jean-Baptiste
, p. 1971 - 1993 (2017/03/20)
Significant work has been dedicated to the discovery of JAK kinase inhibitors resulting in several compounds entering clinical development and two FDA approved NMEs. However, despite significant effort during the past 2 decades, identification of highly s