| 摘要 |
FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to prodrugs of 3-acyl-2-hydroxy- -indole-1-carboxamide of the formula (I) <EMI ID=0.74 HE=54 WI=54 TI=CHI> where R means fragments of the formulas (II) <EMI ID=0.75 HE=21 WI=36 TI=CHI>, (III) <EMI ID=0.76 HE=21 WI=39 TI=CHI>, (IV) <EMI ID=0.77 HE=24 WI=33 TI=CHI>, (V) <EMI ID=0.78 HE=24 WI=36 TI=CHI> and (VI) <EMI ID=0.79 HE=21 WI=21 TI=CHI> where X = 0 or 1; A is C<SB>1-5</SB>--alkylene optionally substituted with 1-2 C<SB>3-7</SB>--cycloalkyls, or phenylene group; B is C<SB>2-5</SB>--alkenylphenyl, pyridyl, piperidinyl, pyrrolidinyl, -OCH<SB>2</SB>CO<SB>2</SB>-R or -OCH<SB>2</SB>CONR<SP>2</SP>R where R - H, alkyl, phenyl-lower alkyl or (CH<SB>2</SB>)<SB>p</SB>CONR<SP>2</SP>R where R and R - H, alkyl or together with bound nitrogen atom they form morpholine group; R and R - H, alkyl, (CH<SB>2</SB>)<SB>p</SB>CO-NR<SP>4</SP>R<SP>3</SP>, (CH<SB>2</SB>)<SB>p</SB>NR<SP>7</SP>R<SP>8</SP>, (CH<SB>2</SB>)<SB>p</SB>OR or (CH<SB>2</SB>)<SB>p</SB>SR where R - H, alkyl, C<SB>3-7</SB>--cycloalkyl optionally substituted with 1-2 alkyl groups, or taken together with a substituent and bound oxygen atom they form tetrahydrofuran ring; R and R - H; R - H or methyl; R and R - halogen; R and R - H, halogen; p = 1-3. Compounds of the formula (I) are enol ester or ether prodrugs of hydroxyindole showing analgetic and antiinflammatory effect. EFFECT: improved method of synthesis, enhanced effectiveness. 15 cl, 1 tbl, 35 ex
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