合成路线:1) By methanolysis of 2,6-dichlorophenylacetonitrile (I) by means of H2SO4 to methyl 2,6-dichlorophenylacetate (II),which is then condensed with guanidine (A) in isopropanol.2) By condensation of S-methylisothiourea (V) with 2,6-dichlorophenylacetyl chloride (VI) in acetone to afford S-methyl-N-(2,6-dichlorophenylacetyl)isothiourea (VII); this product is then treated with ammonia in isopropanol.3) By condensation of 2,6-dichlorophenylacetic acid (VIII) with guanidine (A) in toluene.
参考文献标题:Substituted phenylacetylguanidines: A new class of antihypertensive agents
文献作者:Bream,J.B.; et al.
参考来源:Arzneim-Forsch Drug Res 1975,25(10),1477
合成路线:1) By methanolysis of 2,6-dichlorophenylacetonitrile (I) by means of H2SO4 to methyl 2,6-dichlorophenylacetate (II),which is then condensed with guanidine (A) in isopropanol.2) By condensation of S-methylisothiourea (V) with 2,6-dichlorophenylacetyl chloride (VI) in acetone to afford S-methyl-N-(2,6-dichlorophenylacetyl)isothiourea (VII); this product is then treated with ammonia in isopropanol.3) By condensation of 2,6-dichlorophenylacetic acid (VIII) with guanidine (A) in toluene.
合成路线:4) By reaction of the nitrile (I) with ethyl formate (B) by means of NaOEt in ethanol to give alpha-formyl-2,6-dichlorophenylacetonitrile (III),which is condensed with guanidine hydrochloride (A) by means of NaOEt in ethanol to yield alpha-(guanidinomethylene)-2,6-dichlorophenylacetonitrile (IV); this product is finally hydrolyzed and rearranged by means of HCl.
参考文献标题:BS 100-141
文献作者:Arrigoni-Martelli,E.; Castar,J.
参考来源:Drugs Fut 1976,1(4),167
合成路线:4) By reaction of the nitrile (I) with ethyl formate (B) by means of NaOEt in ethanol to give alpha-formyl-2,6-dichlorophenylacetonitrile (III),which is condensed with guanidine hydrochloride (A) by means of NaOEt in ethanol to yield alpha-(guanidinomethylene)-2,6-dichlorophenylacetonitrile (IV); this product is finally hydrolyzed and rearranged by means of HCl.
参考文献标题:Verfahren zur Herstellung von Acylguanidinen
文献作者:Bream,J.B.; et al.
参考来源:CH 518910
合成路线:4) By reaction of the nitrile (I) with ethyl formate (B) by means of NaOEt in ethanol to give alpha-formyl-2,6-dichlorophenylacetonitrile (III),which is condensed with guanidine hydrochloride (A) by means of NaOEt in ethanol to yield alpha-(guanidinomethylene)-2,6-dichlorophenylacetonitrile (IV); this product is finally hydrolyzed and rearranged by means of HCl.
参考文献标题:Verfahren zur Herstellung von Acylguanidinen
文献作者:Bream,J.B.; et al.
参考来源:CH 511816
产品链接: CAS No. 29110-48-3›› 产品链接: CAS No.29110-47-2››