Abstract: The present invention provides a novel 6-nitroprostaglandin derivatives of the formula (I) ##STR1## wherein A, n, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined in claim 1.The 6-nitroprostaglandin derivatives is useful as medicines because of its excellent pharmacological activities including platelet aggregation inhibiting activity, blood pressure lowering activity and anti-ulcerous activity, and useful as intermediate for other pharmaceutically active compounds such as 6-oxoprostaglandin derivatives, prostaglandin E.sub.1 derivatives, etc.

Abstract: A process for producing prostacyclins of the formula ##STR1## wherein the symbol G.sup.1, R.sup.1, R.sup.2, R.sup.31 and R.sup.41 are as defined in claim 1,which comprises reacting 5,6-dehydroprostaglandins F.sub.2 of the formula ##STR2## wherein the symbol G, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined in claim 1,with a mercury (II) compound in an inert organic solvent in the presence of tri(C.sub.1 -C.sub.6)alkylamine, treating the reaction product with a boron hydride compound, and if necessary, subjecting the reaction product to deprotecting reaction, hydrolysis reaction, or salt-forming reaction.This process is industrially advantageous process for the preparation of prostacyclin and its derivatives.

Abstract: Novel 5- or 7-monohalogenated or 5,7-dihalogenated .sup.6 -PGI.sub.1 and 5- or 7-monohalogenated or dihalogenated PGI.sub.2 (except 5-monofluorinated PGI.sub.2). The novel halogenated prostacyclins are useful for controlling vascular actions and also in organ transplantation, extra-corporeal circulation and the like. The present invention also provides processes for preparing the novel halogenated prostacyclins.

Abstract: A novel compound selected from the group consisting of 7-(or 6- or 4-)thiaprostaglandin E.sub.1 derivatives of the formula (I). ##STR1## wherein A represents --CH.sub.2 -- or ##STR2## in which n is 0, 1 or 2, provided that only one A cut of three is ##STR3## R.sup.1 -R.sup.7 and G are as defined in the specification, the 15-epimers of said thiaprostaglandin E.sub.1 derivatives, the enatiomers of said thiaprostaglandin E.sub.1 derivatives or their 15-epimers, and mixtures of these compounds.A 7-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by reacting a 2-organo-2-cyclopentenone (II) with an organic copper-lithium compound (III) to effect conjugation reaction. A 6-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by subjecting an .alpha.,.beta.-unsaturated ketone (IV) and a thiol (V) to the Michael addition reaction.

Abstract: A compound selected from thiazolo[3,2-a]pyrimidines or their enolate derivatives represented by the following general formula ##STR1## wherein R.sup.1 and R.sup.2 are identical or different, and each represents a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 3 to 10 carbon atoms, a substituted or unsubstituted phenyl group, a substituted or unsubstituted cycloaliphatic group having 3 to 8 carbon atoms, a substituted or unsubstituted phenylalkyl group or a substituted or unsubstituted acyl group having 2 to 7 carbon atoms, provided that R.sup.1 and R.sup.2 are not simultaneously hydrogen atoms or substituted or unsubstituted acyl groups having 2 to 7 carbon atoms; and R.sup.1 and R.sup.2, when taken together, may form, with the nitrogen atom to which they are bonded, a 5- or 6-membered ring which may further contain one or more hetero atoms;and acid addition salts of these compounds.

Abstract: A derivative of thiazolo [3,2-a] pyrimidine expressed by formula (I) ##STR1## (where R indicates a phenyl group or a benzyl group which has a halogen atom, a lower alkyl or lower alkyloxy group as a substituent group, an alicyclic group or an arylethyl group), and a process for the preparation of a compound of formula (I) comprising cyclizing a compound expressed by formula (II) by application of heat ##STR2## (where a definition of R is as same as that given in case of formula (I) and R' indicates a halogen atom or lower alkyloxy group). A drug which contains this compound as active ingredient is useful for curing autoimmune diseases such as rheumatoid arthritis, nephritis, etc.

Abstract: A novel 7-hydroxyprostaglandin E.sub.1, or a stereoisomer thereof, or a protected derivative thereof, having the following formula: ##STR1## wherein R.sup.8 represents H, CH.sub.3 or C.sub.2 H.sub.5, R.sup.9 represents H or CH.sub.3, R.sup.10 and R.sup.11 are identical or different, and each represents H, tetrahydropyranyl or t-butyldimethylsilyl. Also provided is a process for producing an adjacently disubstituted ketone including the above compounds, i.e. 7-oxoprostaglandin, etc. which comprises reacting an .alpha.,.beta.-unsaturated carbonyl compound with a cuprous salt and an organolithium compound in an aprotic inert organic medium in the presence of trialkylphosphine, the amounts of said cuprous salt and said organolithium compound being substantially equimolar, and reacting the product with a protected acetal derivative of an organic carbonyl compound or an aldehyde in the presence of a Lewis acid, if necessary, followed by reacting the product with a proton donor.

Abstract: Novel 1-substituted-3-acylpyrrole derivatives of the formula ##STR1## wherein all symbols are as defined in the specification; and platelet aggregation inhibiting agents comprising them as active ingredients. These novel 1-substituted-3-acylpyrrole derivatives are prepared by condensing the corresponding 1-substituted pyrrole derivatives with the corresponding acylating agents in the presence of acid catalysts, and if desired, subjecting the products to oxidation, hydrolysis, amidation or acetal-forming reaction. These 1-substituted-3-acylpyrrole derivatives exhibit unique properties in that they have superior platelet aggregation inhibiting actions with low antiinflammatory activity.

Abstract: Organothiocyclopentanes of the formula ##STR1## wherein E represents >C.dbd.O or ##STR2## in which Z' represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; X represents --S--, --CH.sub.2 --, --CH.dbd.; represents a single or double bond; R' represents a monovalent or divalent organic group containing 1 to 25 carbon atoms; R represents a monovalent organic group containing 1 to 25 carbon atoms; Z represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; and when both E and Z represent a hydroxyl group or a protected hydroxyl group, X represents --S--.Also, 2-organothio-2-cyclopentenones of the formula ##STR3## wherein R and Z are as defined above. The compounds of formula (I) are prepared by reacting 2,3-epoxy-cyclopentanone or its derivatives with mercaptans in the presence of basic compounds.

Abstract: 1,3-Dicarbonyl compounds useful as medicines, agricultural chemicals, perfumes, and their intermediates are prepared by reacting a specific .alpha.,.beta.-unsaturated carbonyl compound with a specific organic copper lithium compound in the presence of an aprotic inert organic solvent, and then reacting the reaction product with an organic carboxylic acid halide or anhydride. In particular, novel 2-acyl-3-substituted cyclopentan-1-ones and 2-acyl-3-substituted cyclohexan-1-ones having important physiological activities are provided.

Abstract: Novel optically active compounds of 4-protected hydroxy-cyclopent-2-en-1-ones of the formula ##STR1## wherein R is a splittable protective group for an alcoholic hydroxyl group, and a process for preparing the 4-protected hydroxycyclopent-2-en-1-ones by oxidizing monohydroxy-protected derivatives of cyclopent-1-ene-3,5-diol expressed by the following formula ##STR2## wherein R is the same as defined above. Optically active 4-hydroxycyclopent-2-en-1-one which is an optically active isomer of the compound of formula (2); or optically active cyclopent-1-en-3,5-diol (R-isomer) and a novel diacyl derivative of the diol, a novel monoacylmonosilyl-derivative of the diol and a novel monoacylmonotetrahydropyranol-derivative of the diol, which are intermediates for the protective derivative of formula (1). Processes are also provided for preparing the protective derivatives of formula (1) by converting these intermediates by esterification, hydrolysis, enzymatic processes, etc.

Abstract: A process for preparing cyclopent-2-en-1-one derivatives of the formula ##STR1## wherein R.sub.1 is a substituted or unsubstituted alkyl group or a substituted or unsubstituted aryl group, andR.sub.2 is a hydrogen atom or a substituent which is not substantially brominated under the treating conditions, which comprises treating a cyclopentanone derivative of the formula ##STR2## wherein R.sub.1 and R.sub.2 are the same as defined above, with pyridinium hydrobromide perbromide.

Abstract: 1,3-Dicarbonyl compounds useful as medicines, agricultural chemicals, perfumes, and their intermediates are prepared by reacting a specific .alpha.,.beta.-unsaturated carbonyl compound with a specific organic copper lithium compound in the presence of an aprotic inert organic solvent, and then reacting the reaction product with an organic carboxylic acid halide or anhydride. In particular, novel 2-acyl-3-substituted cyclopentan-1-ones and 2-acyl-3-substituted cyclohexan-1-ones having important physiological activities are provided.

Abstract: New optically active cyclopentene-diol and the mono- or diacyl esters thereof and a process for converting a diacyl ester of cyclopent-1-en-3,5-diol to its monoacyl ester and/or its diol which comprises subjecting a diacyl ester of cyclopent-1-en-3,5-diol containing at least one of the optically active or inactive diacyl ester of trans-cyclopent-1-en-3,5-diol (trans-isomer) and diacyl esters of cis-cyclopent-1-en-3,5-diol (cis-isomer), to the action of a microorganism or enzyme having at least a selectivity in its rates of hydrolyzing the acyloxy group (R) configuration and the acyloxy group (S) configuration of said diacyl ester. These new compounds are valuable as starting materials for the preparation of prostaglandin or its analogues.

Abstract: A process for the preparation of 1,4-diacetoxycyclopent-2-ene, which comprises contacting a solution of 1,4-dibromocyclopent-2-ene in an inert organic solvent which is slightly soluble or insoluble in water, with an aqueous solution or suspension of at least one metal salt of acetic acid which is at least partially water-soluble, in the presence of a cationic surface-active compound.