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US 7,119,180 B2Granted
2-halogenated derivatives of 5-O-desosaminyl-erythronolide A, their preparation process and their antibiotic use
AssigneeAventis Pharma S.A.
InventorsConstantin Agouridas, Francois Bretin, Alexis Denis, Claude Fromentin
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Abstract
A subject of the invention is a process for the preparation of the compounds of formula (I): Wherein the substituents are defined as in the application. The compounds of this invention exhibit antibiotic properties.
Claims7
A process for the preparation of a compound of formula (I):
- wherein:
- A is nitrogen or N→O;
- Hal is halogen;
- R1 and R2 are the same or different and are independently chosen from hydrogen or C1–C18alkyl;
- R is —(CH2)mOB;
- wherein
- m is an integer from 1 to 8;
- and
- B is hydrogen, —COAr or —(CH2)n—Ar;
- wherein
- n is an integer from 1 to 8;
- and
- Ar is a mono- or polycyclic aryl or heteroaryl;
- Z is hydrogen or C1–C18-acyl;
- said process comprising:
- reacting a compound of formula (IIIA)
- wherein:
- A, R, R1 and R2 are as defined above;
- and
- M is a hydroxyl protecting group;
- with a suitable halogenating agent to obtain a compound of the formula IB:
- reacting the compound of formula (IB) with a suitable deprotecting agent to obtain the compound of formula (I) wherein Z is hydrogen.
19 more elements
Dependencies are inferred from the claim text.