摘要:
A process for the manufacture of a 6-acyl-7-deacetylforskolin derivative represented by formula (I) ##STR1## by reacting a 7-acyl-7-deacetylforskolin derivative represented by formula (II) ##STR2## with a strong base in an aprotic solvent.
摘要:
This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each stands for an acyl group and R.sup.3 stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.
摘要翻译:本发明涉及一种制备由以下通式表示的6,7-二酰基-7-脱乙酰福斯克林衍生物的方法:(*化学结构*)(I)其中R1和R2各自代表酰基,R3代表 具有2至3个碳原子的脂族基团,其包括通过以下通式除去在通式为(* CHEMICAL STRUCTURE *)(III)表示的1,6,7-三酰基-7-脱乙酰福斯克林衍生物中的第1位的酰基,其中R1 ,R2和R3如上定义,通过溶剂分解。 预期式(I)化合物为药物。
摘要:
This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each stands for an acyl group and R.sup.3 stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.
摘要:
This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each stands for an acyl group and R.sup.3 stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.
摘要:
The present invention relates to novel pharmaceutical use of forskolin derivatives represented by the general formula: ##STR1## wherein R.sup.1, R.sup.2 and Ac are as defined later ##STR2## (wherein R.sup.3 and R.sup.4 are each hydrogen or lower alkyl group, or R.sup.3 and R.sup.4 may be combined to represent lower alkylene group which may have oxygen or nitrogen atom in the linking chain, and n is an integer of 1 to 5); R.sup.2 represents hydrocarbon group having 2 to 3 carbon atoms; and Ac represents acetyl group. The above-mentioned forskolin derivative or a physiologically acceptable salt thereof can be used as a platelet aggregation inhibiting or controlling agent, spasmolytic agent, therapeutic agent for skin ulcer, peripheral circulation improving agent for limbs and differentiation inducing and promoting agent.
摘要:
This invention relates to forskolin derivatives, their physiologically acceptable salts, and a process for producing these compounds. The forskolin derivative is represented by the general formula ##STR1## wherein; I. when R.sup.1 is hydrogen and R.sup.4 is vinyl, ethyl, or cyclopropyl,(1) either of R.sup.2 and R.sup.3 denotes a residue represented by the formula ##STR2## wherein each of R.sup.5 and R.sup.6 denotes hydrogen or lower alkyl or R.sup.5 and R.sup.6 combine with each other to form a lower alkylene chain which may or may not contain an oxygen or nitrogen atom and m is an integer of 1 to 5, and the other one of R.sup.2 and R.sup.3 denotes hydrogen or a residue represented by the formula CO(CH.sub.2).sub.n X, X being hydrogen or ##STR3## wherein, each of R.sup.7 and R.sup.8 denotes hydrogen or lower alkyl or R.sup.7 and R.sup.8 combine with each other to form a lower alkylene chain which may or may not contain an oxygen or nitrogen atom, and n being an integer of 1 to 5, or(2) R.sup.2 denotes hydrogen or --COCH.sub.2 CH.sub.2 CO.sub.2 H and R.sup.3 denotes hydrogen, --COCH.sub.3, --COCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H, or --COCH(OH)CH.sub.2 OH with the proviso that R.sup.3 is one of the last two residues when R.sup.2 is hydrogen, andII. whenR.sup.1 is a residue represented by a formula of CO(CH.sub.2).sub.p CO.sub.2 H and ##STR4## wherein, each of R.sup.9 and R.sup.10 denotes hydrogen or lower alkyl, p is an integer of 0 to 5, and q is an integer of 1 to 5,R.sup.2 denotes hydrogen , R.sup.3 denotes acetyl, and R.sup.4 denotes vinyl.