Guaiacoxypropanolamines with alpha/beta adrenergic blocking activity
AssigneeNational Science Council
InventorIng-Jun Chen
Life of this patent
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Abstract
The invention reveals a novel structure of guaiacoxypropanolamines shown in formula I 1 The composition comprising formula I as active intergant and pharmaceutical acceptable vehicle. The effects of composition by perfect administration routes in the mammal when given potential α/β-adrenergic blocking activity, selective for emergency hypertension.
Claims14
A guaiacoxypropanolamines compound of Formula I, show as follow structure,
- 4
A process for preparing a guaiacoxypropanolamines, which consists of;
- a.) 4-oxyethylamine-3-methoxybenoic acid ethyl ester compound, which is derived from heating 4-hydroxy-3-methoxybenzoic acid ethyl ester and ethylene dibromide and adding sodium hydroxide. Ethylene is mixed with ethyl acid ethyl ester as the diluent;
- silicone filled tube is used for separation. Equal molar of potassium phthalimide is added before heating for reaction, then equal molar of hydrazine hydrate is heated for reaction;
- b.) The compounding of epoxide:
- under alkali ethyl condition, raw materials such as nonivamide and 4—hydroxy-3-methoxy-1-propenylezene are mixed for reaction before adding epichlorohydrine for diffusion;
- upon reaction and pressurized reduction, silicone filled tubing is used for separation to obtain white crystallization;
- c. )The compounding of N-[4- (2hydroxy-3- (4-oxyethylamino-3-methoxy-benzoic acid) propoxy)-3-methoxy] -l-propylenyl benzene:
- amines reaction is achieved through 4-oxyethylamine-3-methoxybenzoic acid ethyl ester and an equal molar of eposide;
- upon placing overnight, crystallization is obtained.
The method claimed as claimed 2, whether
- a.) The compoounding of 4-oxyethylamine-3-methoxycinnamic acid ethyl ester:
- 4-hydroxy-3-methoxycinnamic acid ethyl ester and ethylene dibromide are heated and stirred before adding sodium hydroxide. Ethane is mixed with ethyl acid ethyl ester as the diluent, silicone filled tube is used for separation. After equal molar of potassium phthalimide is added and heated for reaction, equal molar of hydrazine hydrate is heated for reaction;
- b.) The compounding of N-[4(2,3-epoxy-propoxy)-3-methoxy]-1-propenyl benzene:
- Under alkaline condition, 4-hydroxy-3-methoxy-l-propenylbezene is reacted before adding epichlorohydrine for diffusion;
- upon thorough reaction and pressurized reduction, silicone filled tube is used for separation to obtain white crystallization.
- c.) The compounding of N-[4-(2-hydroxy-3-(4-oxyethylamino -3-methoxy-cinnamic acid)propoxy)-3-methoxy]-1-propylenyl benzene:
- amines reaction is achieved with 4- oxyethylamine-3-methoxycinnamic acid ethyl ester and equal molar percentage of epoxide, which is placed overnight to obtain crystallization.
A compound, [(4-allyl-2-methoxy)phenoxy]-3-[2-methoxy - phenoxyethyl) amino] -propanol.
A compound,[(4-nonanamide-2-methoxy)phenoxy]-3-[(2-methoxyphenoxytheyl)amino]-propanol.
A compound, 1-[(4-propenoic acid ethyl ester-2-methoxy)phenoxy]-3-[(2-methoxyphenoxy-ethyl)amino]-propanol.
A compound, 1-[(4-propenyl-2-methoxy)-phenoxy]-3-[(2-methoxyphenoxyethyl)amino]-propanol.
A compound, N- [4- (2-hydroxy-3- (4-oxyethylamino-3-methoxycinnamic acid)propoxy)-3-methoxy]-1-propylenyl-benzene.
A compound, N—[4-(2-hydroxy-3-(4-oxyethyl-aminnon-3-methoxybenzoic acid)propoxy)-3-methoxybenzyl]-nonanamide.
A compound, N-[4-(2-hydroxy-3-(4-oxyethyl amino-3-methoxybenzoid acid)propoxy)-3-methoxy]-1-propenylbenzene.
A compound, N-[4-(2-hydroxy-3-(4-oxyethylamino-3-methoxycinnamic acid)propoxy)-3-methoxybennzyl]-nonanamide.
A compound, N-[4-(2-hydroxy-3-(1-oxyethyl amino-4-oxyacetic acid benzene)propoxy)-3-methoxy]-1-propenylbenzene.
A compound, N-[4-(4-ethylamino-1-oxyacetic acid benzene ethoxy]-1-oxyacetic acid ethyl ester benzene.
Dependencies are inferred from the claim text.