PROCESS FOR PREPARING SELECTIVE BIOLOGICALLY ACTIVE 7-OXO-PROSTACYCLINE DERIVATIVES
Title compds. I [R1=C1-4 alkyl; R2=H, C1-4 alkanoyl; A=ethylene, vinylene; n=2,3,4 are prepd. Thus, 340mg methyl ester of 7-oxo- 16,17,18,19,20-pentanor-15-cyclopentyl-PGI2 in 50ml methanol is treated with 0.5ml 1mol-sodium methoxide and stirred at room temp. for 10h. After --20ml MetOH is removed,...
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Zusammenfassung: | Title compds. I [R1=C1-4 alkyl; R2=H, C1-4 alkanoyl; A=ethylene, vinylene; n=2,3,4 are prepd. Thus, 340mg methyl ester of 7-oxo- 16,17,18,19,20-pentanor-15-cyclopentyl-PGI2 in 50ml methanol is treated with 0.5ml 1mol-sodium methoxide and stirred at room temp. for 10h. After --20ml MetOH is removed, the resulting mixt. is treated with 5ml 1N-NaOH at 40 C for 3h. After the MetOH is removed, the resulting ppt. is dissolved in 20ml H2O. extd. with ether, adjusted to PH=6.0 with 1N-NaHSO4 and extd. with ethyl acetate. After the upper layer is adjusted to PH=4.0 with NaHSO4 at 0 C and extd. with ethyl acetate, all the ethyl acetate layer is washed with satd. NaCl. |
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