合成路线:Dazopride can be prepared by the condensation of the 1,2-diethyl-4-aminopyrazolidine (VIII) with either 4-amino-5-chloro-2-methoxybenzoic acid in the presence of phosphorus trichloride-pyridine or the corresponding mixed anhydride (IX).
参考文献标题:N-(4-Pyrazolidinyl)benzamides and their amino precursors
文献作者:Cale,A.D.Jr.; Lunsfod,C.D.(A.H.Robins Co.Inc.)
参考来源:US 4207327
合成路线:The dialkylation of aqueous N,N'-diacetyl-hydrazine by simultaneous addition of diethyl sulfate and potassium hydroxide so as to maintain a pH of 10.5-11.5 affords N,N'-diacetyl-N,N'-diethylhydrazine,which is hydrolyzed to diethylhydrazine (II) by hydrochloric acid.The pH of the acid solution is adjusted to 10,where it is maintained during the addition of epichlorohydrin to give 1,2-diethyl-4-pyrazolidinol (III).The pyrazolidinol is converted to 1,2-diethyl 4-aminopyrazolidine (VIII) by either amination of the corresponding chloro compound (IV) or displacement of the mesyloxy group in compound (V) by the azide ion,followed by reduction.
参考文献标题:Process for the preparation of 4-Pyrazolidinols
文献作者:Cale,A.D.Jr.; Jenkins,H.(A.H.Robins Co.Inc.)
参考来源:DE 2031489; ES 380355; FR 2053022; GB 1309018; US 3660426
合成路线:The dialkylation of aqueous N,N'-diacetyl-hydrazine by simultaneous addition of diethyl sulfate and potassium hydroxide so as to maintain a pH of 10.5-11.5 affords N,N'-diacetyl-N,N'-diethylhydrazine,which is hydrolyzed to diethylhydrazine (II) by hydrochloric acid.The pH of the acid solution is adjusted to 10,where it is maintained during the addition of epichlorohydrin to give 1,2-diethyl-4-pyrazolidinol (III).The pyrazolidinol is converted to 1,2-diethyl 4-aminopyrazolidine (VIII) by either amination of the corresponding chloro compound (IV) or displacement of the mesyloxy group in compound (V) by the azide ion,followed by reduction.
合成路线:An alternative method of producing the 1,2-diethyl-4aminopyrazolidine (VIII) is by reduction of the corresponding nitro compound (VII),which is derived from 1,3-dimorpholino-2-nitropropane (VI) and 1,2-diethylhydrazine (II).
合成路线:Dazopride can be prepared by the condensation of the 1,2-diethyl-4-aminopyrazolidine (VIII) with either 4-amino-5-chloro-2-methoxybenzoic acid in the presence of phosphorus trichloride-pyridine or the corresponding mixed anhydride (IX).
参考文献标题:Dazopride succinate
文献作者:Cale,A.Jr.
参考来源:Drugs Fut 1985,10(7),553
合成路线:The dialkylation of aqueous N,N'-diacetyl-hydrazine by simultaneous addition of diethyl sulfate and potassium hydroxide so as to maintain a pH of 10.5-11.5 affords N,N'-diacetyl-N,N'-diethylhydrazine,which is hydrolyzed to diethylhydrazine (II) by hydrochloric acid.The pH of the acid solution is adjusted to 10,where it is maintained during the addition of epichlorohydrin to give 1,2-diethyl-4-pyrazolidinol (III).The pyrazolidinol is converted to 1,2-diethyl 4-aminopyrazolidine (VIII) by either amination of the corresponding chloro compound (IV) or displacement of the mesyloxy group in compound (V) by the azide ion,followed by reduction.
合成路线:Dazopride can be prepared by the condensation of the 1,2-diethyl-4-aminopyrazolidine (VIII) with either 4-amino-5-chloro-2-methoxybenzoic acid in the presence of phosphorus trichloride-pyridine or the corresponding mixed anhydride (IX).
参考文献标题:Synthetic and pharmacological properties of N-(1,2-dialkyl-4-pyrazolidinyl)benzamides - Selective gastric prokinetic agents
文献作者:Munson,H.R.Jr.; Cale,A.D.Jr,Lo,Y.S.; Lunsford,C.D.
参考来源:187th ACS Natl Meet (April 8-13,St.Louis) 1984,7(9),650
产品链接: CAS No. 70181-03-2›› 产品链接: CAS No.81957-25-7››