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Processes for preparing macrolides and ketolides and intermediates for them
专利权人:
Cempra Pharmaceuticals; Inc.
发明人:
PEREIRA, David
申请号:
ES11784318
公开号:
ES2636948T3
申请日:
2011.05.20
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A process for preparing a compound of the formula (I), ** (See formula) ** or a pharmaceutically acceptable salt thereof, wherein: R 10 is hydrogen or acyl; X is H; and Y is OR7; wherein R7 is monosaccharide, disaccharide, alkyl, arylalkyl or heteroarylalkyl, each of which is optionally substituted, or acyl or C (O) NR8R9; where R8 and R9 are each independently selected from the group consisting of hydrogen, hydroxy, alkyl, heteroalkyl, alkoxide, aryl, arylalkyl, heteroaryl and heteroarylalkyl, each of which is optionally substituted, and dimethylaminoalkyl, acyl, sulfonyl, ureido and carbamoyl ; or R8 and R9 are taken together with the attached nitrogen to form an optionally substituted heterocycle; or X and Y are taken together with the carbon attached to form carbonyl; V is C (O), C (>; = NR11), CH (NR12R13), or N (R14) CH2; where N (R14) is adhered to C-10 carbon; where R11 is hydroxy or alkoxide; R12 and R13 are each independently selected from the group consisting of hydrogen, hydroxy, alkyl, alkoxide, heteroalkyl, aryl, arylalkyl, heteroaryl, and heteroarylalkyl, each of which is optionally substituted, and dimethylaminoalkyl, acyl, sulfonyl, ureido and carbamoyl ; R14 is hydrogen, hydroxy, alkyl, alkoxide, heteroalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl, each of which is optionally substituted, or dimethylaminoalkyl, acyl, sulfonyl, ureido or carbamoyl; W is H, F, Cl, Br, I, or OH; A is CH2, C (O), C (O) O, C (O) NH, S (O) 2, S (O) 2NH, or C (O) NHS (O) 2; B is (CH2) n where n is an integer from 0 to 10; or an unsaturated carbon chain of 2 to 10 carbons; and C is hydrogen, hydroxy, alkyl, alkoxide, heteroalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl, each of which is optionally substituted, or acyl, acyloxide, sulfonyl, ureido, or carbamoyl; the process comprising ** (See formula) ** ...Un procedimiento para preparar un compuesto de la fórmula (I), **(Ver fórmula)** o una sal farmacéuticamente aceptable de la misma, donde: R10 es hidr
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