215316-49-7Relevant academic research and scientific papers
Process for the synthesis of an antiviral compound
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Page 10-11, (2010/02/07)
In a process comprising synthesizing pyranes including [R—(R*,R*)]-N-[3-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide the present invention comprises the improvements comp
Process for asymmetric hydrogenation
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, (2008/06/13)
The present invention is a process for the preparation of a compound of the formula: where R3, R4 and n are defined in the specification which comprises hydrogenating a compound of the formula: the E-geometrical isomer thereof or a mixture of the Z- and E-isomers in the presence of catalyst containing Rh, a chiral ligand with at least one phosphorous atom where the hydrogenation is conducted in the presence of a base.
Process to produce a protease inhibitor
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, (2008/06/13)
Disclosed is a novel process and novel intermediates to prepare [R-(R*,R*)]-N-[3-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide (XIX) which is a protease inhibitor useful in treating humans infected with the HIV virus.
A convergent, scalable synthesis of HIV protease inhibitor PNU-140690
Fors, Kristina S.,Gage, James R.,Heier, Richard F.,Kelly, Robert G.,Perrault, William R.,Wicnienski, Nancy
, p. 7348 - 7356 (2007/10/03)
PNU-140690, an inhibitor of the HIV protease enzyme undergoing clinical evaluation as a chemotherapeutic agent for treatment of AIDS, was synthesized by a convergent approach amenable to large-scale preparation in a pilot plant environment. The key step is the aldol addition of nitroaromatic ester (+)-8 to aldehyde 19e. The two stereocenters present in the target molecule were each set independently by resolution of enantiomers. Intermediates along the synthetic routes were chosen to maximize opportunities for isolation and purification by crystallization.
