- Solid-phase synthesis of N,N′-substituted acylguanidines
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An efficient method for the solid-phase synthesis of N,N′-substituted acylguanidines is presented. The key-step involves the N-acylation of resin immobilized S-methylisothiourea with a variety of carboxylic acids using PyAOP as the coupling agent. The resulting resin bound N-acyl-derivatives are reacted with a host of amines and the N-acyl,N′-alkyl(aryl)guanidines liberated from the resin upon exposure to TFA.
- Dodd, Dharmpal S.,Zhao, Yufen
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- The preparation method of the overall tablet sizes hydrochloride (by machine translation)
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The invention discloses a method for preparing the acid salt of the overall tablet sizes. In order to 2, 6 - dichloro acetic acid and methoxy isourea hydrochloride as the starting material, by catalytic condensation, aminolysis, salt, purifying to obtain the hydrochloric acid overall tablet sizes. The preparation method of mild reaction conditions, the operation is simple, compared with the prior art, reduce the operation step, reducing the total reaction time, reduce energy consumption, pollution is smaller, is beneficial to the environment. (by machine translation)
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Paragraph 0027; 0028; 0029
(2017/08/29)
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- Substituted phenylacetylguanidines: a new class of antihypertensive agents
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The synthesis of a new series of phenylacetylguanidines is described. Several of them exhibited high antihypertensive activity in the rat. The most potent member of the series is N amidino 2 (2,6 dichlorophenyl) acetamide hydrochloride [2,6 dichlorophenylacetylguanidine hydrochloride, compound 19], which is now in clinical study under the clinical code number BS 100-141. The structure activity relationships in this class of compounds are discussed.
- Bream,Lauener,Picard,Scholtysik,White
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p. 1477 - 1482
(2007/10/05)
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