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Application filed by Merrell Pharma IncfiledCriticalMerrell Pharma Inc
Priority claimed from PCT/US1995/004399external-prioritypatent/WO1995029932A1/en
Publication of MXPA96005321ApublicationCriticalpatent/MXPA96005321A/en
Publication of MX9605321ApublicationCriticalpatent/MX9605321A/en
Preparation Of Compounds By Using Micro-Organisms
(AREA)
Steroid Compounds
(AREA)
Abstract
The present invention provides 4-nitro-'DELTA'4-3-ketosteroids, their use as steroid C17-20 lyase and 5'alpha'-reductase inhibitors and to a novel process for preparing a compound of formula (I), comprising sequentially: a) reacting a starting compound of formula (II) with an effective amount of a strong base at an elevated or suitable temperature for a time sufficient to create the corresponding thermodynamic dienolate, followed by addition of a neutral nitrating agent to produce the 4-nitro-steroid; and then, b) reacting the 4-nitrosteroid with a suitable reducing agent.
MX9605321A1995-04-111995-04-11Process for the preparation of 4-amino-'delta'4-3-ketosteroids via 4-nitro-'delta'4-3-ketosteroids.
MX9605321A
(en)
NOVEL OCTAHYDRO-6,10-DIOXO-6H-PYRIDAZINO/1,2-a/ /1,2/DIAZEPIN-1-CARBOXYLIC ACID DERIVATIVES, PREPARATION METHOD AND USE FOR PREPARING THERAPEUTICALLY ACTIVE COMPOUNDS
A process for making a clinically efficacious HIV protease inhibitor eliminates one step in its synthesis, by an alternative convergent synthesis using 2(S)-4-picolyl-2-piperazine-t-butyl-carboxamide as an intermediate.