73996-31-3Relevant academic research and scientific papers
Facile synthesis of 6a-carbaprostaglandin I2
Konishi, Yoshitaka,Kawamura, Masanori,Iguchi, Yoichi,Arai, Yoshinobu,Hayashi, Masaki
, p. 4391 - 4399 (2015/01/08)
The optically active 6a-carbaprostaglandin I2 (2), a stable mimic of natural prostacyclin (1), was synthesized from the lactone 4 or the hydroxy acid 5, which were general synthetic intermediates for natural prostaglandins.
Novel prostacyclin derivatives and a process for the preparation thereof
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, (2008/06/13)
Compounds of the formula STR1 wherein R1 is (a) hydrogen, (b) C1-10 alkyl, (c) C1-10 alkyl substituted by halogen; C1-4 alkoxy; C6-10 aryl; C6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group; di-C1-4 -alkylamino; or tri-C1-4 -alkylammonium, (d) C4-10 cycloalkyl, (e) C4-10 cycloalkyl substituted by C1-4 alkyl, (f) C6-10 aryl, (g) C6-10 aryl substituted by 1-3 halogen atoms, a phenyl group 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group, or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S; A is --CH2 --CH2 --, trans--CH=CH-- or --C C--; W is hydroxymethylene, RO-methylene, CH3 or CH3, STR2 wherein OH or OR is in the α- or β-position and R is an in vivo hydrolyzable and physiologically acceptable ether or acyl group which is conventional for modifying OH groups in prostaglandins; D and E together are a direct bond, or D is C1-10 alkylene, C1-10 alkenylene or C1-10 alkynylene or one of these groups substituted by fluorine, and E is oxygen, --C C-- or a direct bond; R2 is (a) a C1-10 hydrocarbon aliphatic radical, (b) a C6-10 hydrocarbon aliphatic radical substituted by C6-10 aryl or by C6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group; (c) C4-10 cycloalkyl, (d) C4-10 cycloalkyl substituted by C1-4 alkyl, (e) C6-10 aryl, (f) C6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group; or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S; and R3 is OH or OR; and, when R1 is hydrogen, the salts thereof with physiologically compatible bases, are effective as antihypertensive, bronchiodilators, thrombocyte aggregation inhibitors, inter alia.
Facile synthesis of 6a-carbaprostaglandin I2
Konishi, Yoshitaka,Kawamura, Masanori,Iguchi, Yoichi,Arai, Yoshinobu,Hayashi, Masaki
, p. 4391 - 4399 (2014/12/10)
The optically active 6a-carbaprostaglandin I2 (2), a stable mimic of natural prostacyclin (1), was synthesized from the lactone 4 or the hydroxy acid 5, which were general synthetic intermediates for natural prostaglandins.
