921598-21-2

Upstream product

• 107-14-2 chloroacetonitrile 
• 17356-08-0 thiourea 
• 154848-44-9 4'-hydroxy-3-biphenylcarbonitrile 
• 808769-20-2 3'-(aminomethyl)biphenyl-4-ol 
• 36076-19-4 dimethyl 2,2'-(1,3-phenylene)diacetate 
• 626-16-4 3-(chloromethyl)benzyl chloride 
• 106-41-2 4-bromo-phenol 
• 150255-96-2 (3‐cyanophenyl)boronic acid 
• 865589-70-4 [3-(2-tert-butoxycarbonylamino-2-methylpropyl)phenyl]acetic acid 
• 921598-16-5 ethyl [3-(2-tert-butoxycarbonylamino-2-methylpropyl)phenyl]acetate 
• 921598-18-7 {3-[2-(2,2,2-trichloro-acetylamino)-2-methyl-propyl]-phenyl}-acetic acid 
• 861448-90-0 ethyl 2-[3-(2-amino-2-methylpropyl)phenyl]acetate hydrogen (2R,3R)-2,3-bis[(4-methylbenzoyl)oxy]succinate 
• 865589-97-5 3'-(aminomethyl)biphenyl-4-ol hydrochloride 
• 808768-96-9 2-[3-(2-hydroxy-2-methylpropyl)phenyl]acetic acid 

Downstream Products

• 921598-25-6 2-(3-{2-[((2R)-2-{4-benzyloxy-3-[(methylsulfonyl)amino]phenyl}-2-{[tert-butyl(dimethyl)silyl]oxy}ethyl)amino]-2-methylpropyl}phenyl)-N-[(4'-hydroxybiphenyl-3-yl)methyl]-acetamide 
• 921598-22-3 2-[3-(2-{[(2R)-2-{4-(benzyloxy)-3-[(methylsulfonyl)amino]-phenyl}-2-hydroxyethyl]amino}-2-methylpropyl)phenyl]-N-[(4'-hydroxybiphenyl-3-yl)methyl]acetamide 
• 862540-80-5 2-[3-(2-{[(2R)-2-{[tert-butyl(dimethyl)silyl]oxy}-2-{4-hydroxy-3-[(methylsulfonyl)amino]phenyl}ethyl]amino}-2-methylpropyl)phenyl]-N-[(4'-hydroxybiphenyl-3-yl)methyl]acetamide 

Relevant academic research and scientific papers

Inhibitors of nedd8-activating enzyme

The invention relates to an administration unit comprising crystalline form I of {(1 S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate (I-216) hydrochloride salt and to a packaging comprising the administration unit according to the invention.

Optimization of the manufacturing route to PF-610355 (1): Synthesis of intermediate 5

Tertiary carbinamine 5 is an isolated intermediate in the synthesis of a novel, inhaled β-2 adrenoreceptor agonist PF-610355. Process development for the key amide-formation and Ritter reactions, together with reaction understanding studies are discussed in context of the synthesis of 5. The optimized process employed to manufacture 140 kg of 5 is described, and was shown to have superior metrics to the preliminary commercial route.

INTERMEDIATE AND PROCESS FOR THE PREPARATION OF A SULFONAMIDE DERIVATIVE

The invention relates to a crystalline form of 2-chloro-N-{2-[3-(2-{[(4'-hydroxybiphenyl-3- yl)methyl]amino}-2-oxoethyl)phenyl]-1,1-dimethylethyl}acetamide, a process for preparing the same and its use in the preparation of the ?2 agonist N-[(4'-hydroxybiphenyl-3- yl)methyl]-2-(3-{2-[((2R)-2-hydroxy-2-{4-hydroxy-3- [(methylsulfonyl)amino]phenyl}ethyl)amino]-2-methylpropyl} phenyl)acetamide which is useful in the treatment of respiratory diseases.

Development of a potential manufacturing route to PF-00610355: A novel inhaled β2-adrenoreceptor agonist

The development of a practical, scalable route to PF-00610355 (8) is described. In this convergent approach, amine 9 is coupled to protected bromohydrin 1 to give the doubly protected intermediate 26. TBS-Deprotection of 26 affords the benzyl protected pe

PROCESS FOR THE PREPARATION OF SULFONAMIDE DERIVATIVES

The invention relates to a process for the preparation of compounds of formula (I) wherein Q1 is a group selected from formulae (II and (III) and a group *-NR6 -Q2-A or, if appropriate, their pharmaceutically acceptable sa