Novel process for preparation of corticosteroids
AssigneeCoral Drugs Pvt. Ltd.
InventorsVinayak TRIPATHI, Rajesh KUMAR, Rohit BHUWANIA, Binay Kumar BHUWANIA
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Abstract
The present invention discloses a process for the preparation of pregnadiene derivatives having formula I, their stereoisomer and intermediate thereof. Formula I wherein each substituent is independently, R1 and R2 is hydrogen or C1-C8 straight, branched alkyl chain, saturated or unsaturated cycloalkyl; R3 is hydrogen or wherein R5 represents C1-C8 straight, branched alkyl chain or cycloalkyl; R4 is hydrogen or halogen; R6 is hydrogen or halogen;
Claims9
A novel process for the preparation of pregnadiene derivatives of formula I, their stereoisomer and intermediate thereof.
- wherein
- R1 and R2 is independently hydrogen or C1-C8 straight, branched alkyl chain, saturated or unsaturated cycloalkyl;
- R3 is hydrogen or
- R5 represents C1-C8 straight, branched alkyl chain or cycloalkyl;
- R4 and R6 is independently hydrogen or halogen;
- comprising the steps of:
- i. epoxidation of compound of formula II to obtain 9,11-oxido derivative of compound of formula III;
- ii. dihydroxylation and optional fluorination of compound of formula III to obtain compound of formula IV with a proviso when R6 is F.
- iii. epoxide ring opening of compound of formula IV followed by acetalisation to obtain compound of formula V and optionally, debromination of compound of formula V with a proviso R4 is Br to obtain compound of formula V when R4 is H
- iv. deacetylation of compound of Formula V to obtain compound of formula I
A process for preparation of pregnadiene derivatives of Formula A
- wherein
- R3 is hydrogen or
- R5 represents C1-C8 straight, branched alkyl chain or cycloalkyl;
- R4 is halogen;
- comprising the steps of:
- i. epoxidation of compound of formula II to obtain 9,11-oxido derivative of compound of formula III;
- ii. dihydroxylation of compound of formula III to obtain compound of formula IV
- iii. epoxide ring opening of compound of formula IV followed by acetalisation to obtain compound of formula V
- iv. deacetylation of compound of Formula V to obtain compound of formula I
Dependencies are inferred from the claim text.