905587-30-6

Upstream product

• 905587-31-7 (S)-N-(1-(5-fluoropyrimidin-2-yl)ethyl)acetamide 
• 905587-32-8 N-(1-(5-fluoropyrimidin-2-yl)vinyl)acetamide 
• 905587-44-2 1-(5-fluoropyrimidin-2-yl)ethan-1-one 
• 38275-55-7 5- fluoropyrimidine-2-carbonitrile 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 935666-88-9 AZD1480 
• 1079275-47-0 N2-(5-ethoxy-1H-pyrazol-3-yl)-N6-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-3-nitropyridine-2,6-diamine 
• 1079274-94-4 (S)-N-(1-(5-fluoropyrimidin-2-yl)ethyl)-3-(5-isopropoxy-1H-pyrazol-3-yl)-3H-imidazo[4,5-b]pyridin-5-amine 
• 935667-21-3 (1S)-1-(5-fluoropyrimidin-2-yl)ethanamine monohydrochloride 

Relevant academic research and scientific papers

Efficient synthesis of (S)-1-(5-fluoropyrimidin-2-yl)ethylamine using an ω-transaminase biocatalyst in a two-phase system

Screening of 60 transaminases using three different amine donors found that the ω-transaminase from Vibrio fluvialis together with (S)-α-methylbenzylamine to be the most promising combination to deliver the desired (S)-1-(5-fluoropyrimidin-2-yl)-ethylamine (2) in almost quantitative conversion. The process was further improved by the addition of immiscible organic solvents with toluene identified as most suitable concerning the distribution of the reactants without negatively impacting the performance of the biocatalyst. Further process optimization using commercial enzyme preparations of V. fluvialis led to product/catalyst ratios of 15 g/g cell dry weight. This approach led to a process that provided (S)-1-(5-fluoropyrimidin-2- yl)ethylamine (2) in 77% yield with 99.8% ee. In addition, a recombinant E. coli-based whole-cell biocatalyst was also designed and applied to this process. The use of this low cost enzyme formulation gave product of similar quality to that obtained using the commercial formulation of V. fluvialis. This process was further optimized and scaled-up to deliver (S)-1-(5-fluoropyrimidin-2-yl) ethylamine (2)with a yield of 66% and an optical purity of 97.3% ee. These results confirm the efficiency and competitiveness of the transaminase technology for the production of chiral amines.

Use of ω-transaminase enzyme chemistry in the synthesis of a JAK2 kinase inhibitor

ω-Transaminase enzyme chemistry provides an excellent methodology to build synthetically useful chiral amines from their corresponding ketones. An application of this methodology, providing a long-term commercial manufacturing route to a JAK2 kinase inhibitor, is reported herein.

2-(IMIDAZ0LYLAMIN0)-PYRIDINE DERIVATIVES AND THEIR USE AS JAK KINASE INHIBITORS

The present inv ention relates to compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein Ring A is 5- or 6-membered heteroaryl, wherein said 5- or 6-membered heteroaryl is optionally substituted on carbon with one or more R6

HETEROCYCLIC JAK KINASE INHIBITORS

The present invention relates to compounds of Formula (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer

TRICYCLIC 2,4-DIAMIN0-L,3,5-TRIAZINE DERIVATIVES USEFUL FOR THE TREATMENT OF CANCER AND MYELOPROLIFERATIVE DISORDERS

The present invention relates to compounds of Formula (I): (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer.

Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors

The design, synthesis and biological evaluation of a series of pyrazol-3-ylamino pyrazines as potent and selective JAK2 kinase inhibitors is reported, along with the pharmacokinetic and pharmacodynamic properties of lead compounds.

PYRAZOLYL-AMINO-SUBSTITUTED PYRIMIDINES AND THEIR USE FOR THE TREATMENT OF CANCER

The present invention relates to compounds of Formula (I) and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.

PYRAZOLYL-AMINO-SUBSTITUTED PYRAZINES AND THEIR USE FOR THE TREATMENT OF CANCER

The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These novel compounds provide a treatment for myeloproliferative disorders and cancer.

5-AMINOPYRAZOL-3-YL-3H-IMIDAZO [4,5-B] PYRIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER

The present invention relates to compounds of Formula (I) and to their pharmaceutical compositions, and to their methods of use. These novel compounds provide a treatment for myeloproliferative disorders and cancer.

9- (PYRAZOL- 3 -YL) - 9H- PURINE-2 -AMINE AND 3- (PYRAZ0L-3-YL) -3H-IMIDAZ0 [4, 5-B] PYRIDIN-5-AMINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER

The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.