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.
Content, Stephane,Dupont, Thomas,Fedou, Nicolas M.,Smith, Julian D.,Twiddle, Steven J. R.
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.
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(2013/03/26)
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
De Koning, Pieter D.,Castro, Nieves,Gladwell, Iain R.,Morrison, Natalie A.,Moses, Ian B.,Panesar, Maninder S.,Pettman, Alan J.,Thomson, Nicholas M.
p. 1256 - 1265
(2012/02/05)
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
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Page/Page column 42-43
(2010/11/25)
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Get Best Price for921598-25-62-(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