- C-S bond-forming reactions of barbiturylbromide with isothiocarbamides in aqueous media
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The C-S cross coupling of pharmaceutically active barbituric acid derivatives has been achieved by the interaction of selective monobromobarbituric acid with thioureas in an aqueous medium. This method is applicable for simple thiourea as well as monosubstituted thioureas, and corresponding products are obtained in good yield. [Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications for the following free supplemental resource(s): Full experimental and spectral details.]
- Sontakke, Madhuri M.,Jichkar, Atul A.,Dhonde, Madhukar G.,Bhaskar, Chandrakant S.,Berad, Baliram N.
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supporting information
p. 340 - 345
(2014/01/06)
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- Bicyclic compounds
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Substituted N-substituted alkoxyphenyl compounds, compositions containing them, and methods of making and using them.
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- BORONIC ACID AND ESTER INHIBITORS OF THROMBIN
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Novel boronic acid and ester and carboxyl-modified amino acid compounds of the Formula I, which are inhibitors of trypsin-like enzymes, are disclosed:R 1--Z--CHR 2--A, where R 1, Z, R 2 and A are defined within.
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- [3H,7H]thiazolo[3,4-a]pyridines with antiasthmatic and antiinflammatory actions on the respiratory tract
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Compounds of formula (I) STR1 wherein R is an alkyl group; R1 is a cyano, carboxy, alkoxycarbonyl or hydroxylaminocarbonyl group; R2 is substituted or unsubstituted phenyl (C3 -C7)-cycloalkyl, α-, β- or γ-pyridy
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- Process for preparation of enantiomerically pure polysubstituted 1,4-dihydropyridines
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A process for the optical resolution of racemic 1,4-dihydropyridines, containing isothioureido groups. Salification of racemic isothioureas with optically active acids produces diasteroisomeric mixtures of isothiouronium salts, that, using conventional techniques, are separated in the individual components to give optically pure isothioureides of 1,4-dihydropyridines and salts thereof with conventional acids. Said optically pure 1,4-dihydropyridines can then be subjected to desulphuration and to different transformations to give to other enantiomerically pure and therapeutically useful 1,4-dihydropyridines.
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- 2-thiomethyl-substituted-1,4-dihydropyridines, method for their preparation and pharmaceutical compositions containing them
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Compounds of formula I STR1 wherein R1 is an alkoxycarbonyl group, acetyl, benzoyl, cyano, nitro or aminocarbonyl; R2 is an optionally substituted aryl or hetaryl group; R3 is an alkoxycarbonyl group; φ is a thio residue such as alkylthio, cycloalkylthio, arylthio, heteroarylthio, aminoalkylthio, are described. Compounds I are useful in human therapy as antihypertensive, antiulcer, antithrombotic, antiischaemic agents.
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- GUANIDINE CARBOXYLIC ACID ESTERS AND PHARMACEUTICAL PREPARATIONS CONTAINING THESE COMPOUNDS
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New guanidine carboxylic acid esters corresponding to the general formula I STR1 and a process for the preparation of these compounds are described. The compounds according to the invention are H. sub.2-agonists optionally having an additional H 1-antagonistic component. They are distinguished by their improved oral activity. The use of the above-mentioned guanidine carboxylic acid esters and of pharmaceutical preparations containing these esters is also described.
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- Phenylcarbodiimides, compositions containing them and their use in the control of pests
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Novel substituted phenyl-thioureas, -isothioureas and -carbodiimides of formula I STR1 in which R1 is C1 -C8 alkyl, C1 -C8 alkyl mono- or poly-substituted by halogen and/or by C1 -C6/
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- High potency sweetening agents
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Substituted guanidines containing a tetrazole moiety are provided as high potency sweetening agents.
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- Antihypertensive substituted derivatives of 2,5-diamino 1,4-diazole
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This invention relates to new chemical compounds which are derivatives of 2,5-diaminodiazoles. It relates more particularly to new 2-amino 5-(aralkylamino piperidino alkyl) diazoles. These compounds and the acid addition salts thereof have interesting therapeutical properties, particularly anti-hypertensive properties which make them useful as active ingredient of pharmaceutical compositions.
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- Antihypertensive cyanoguanidines
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This invention relates to novel tri-substituted guanidines linked to a piperidine ring. More specifically, it relates to cyanoguanidines of formula I STR1 wherein R1, R2, R3, R4 are substituents n is an integer of zero to 1 n' is an integer of zero to 1 A and B are --CH2 --, CHOH, --CO-- or a single bond as well as the acid addition salts thereof with a mineral or organic acid. The compounds have interesting pharmacological properties which make them useful as active ingredient of medicines, e.g. antihypertensives.
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- N-Heterocyclyl-N-cyano-N-(heterocyclythioalkyl)-guanidines
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Compounds of formula I and salts thereof which are orally pharmacologically active as inhibitors of gastric secretion are disclosed.
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