The invention provides a preparation method of iprolol hydrochloride. The method comprises the following steps: reacting thionyl chloride and methanol to prepare methyl chloride. Methyl p-hydroxyphenylpropionic acid methyl ester is prepared by substitution reaction of p-hydroxyphenylpropionic acid and methyl chlorite. The etherification reaction of methyl hydroxy phenylpropionic acid methyl ester and epichlorohydrin is prepared to obtain 3 - [4 - (2, 3 - epoxypropoxy] phenylpropionic acid methyl ester. 3 - [4 - (2, 3 - Epoxypropoxy] phenylpropionic acid methyl ester and isopropylamine undergo amination reaction to prepare the ilomolol. Diaprolol hydrochloride and hydrochlorination of hydrogen chloride to obtain ilomolol hydrochlorideThe method has the advantages of easily available raw materials, low cost and simple preparation method. The target product has high yield, high purity and market competitiveness.
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Paragraph 0053; 0057-0059; 0060; 0064-0066
(2021/10/11)
Hitting a soft drug with a hard nucleophile: Preparation of esmolol's metabolite by treatment with bis(tributyltin) oxide
A facile method for the production of esmolol's metabolite in high purity is described. Bis(tributyltin) oxide is used to disrupt esmolol's ester linkage, and hydrolysis is completed by addition of water, which also allows the inorganic side products to be conveniently extracted into ether. Evaporation of the aqueous phase and trituration with ethyl acetate provides the carboxylic acid-amine internal salt as a white, free-flowing powder. Taylor & Francis Group, LLC.
Zhang, Cunyu A.,Erhardt, Paul W.
scheme or table
p. 722 - 726
(2012/01/13)
IMAGE-GUIDED THERAPY OF MYOCARDIAL DISEASE: COMPOSITION, MANUFACTURING AND APPLICATIONS
Compositions and methods for imaging and for chemotherapy and radiotherapy are disclosed. More particularly, the invention concerns agents comprising a targeting moeity comprising a beta-adrenergic receptor targeting compound conjugated or embedded with ethylenediamine. The present invention also concerns methods of application of such agents for imaging and treatment of cardiovascular diseases, and kits for preparing a radiolabeled therapeutic or diagnostic agent.
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Page/Page column 12-13
(2009/10/01)
METHOD FOR TREATMENT OR PROPHYLAXIS OF CARDIAC DISORDERS
A method for the treatment of prophylaxis of cardiac disorders in a mammal, comprising administering to such mammal a short-acting β-blocking compound of the formula: STR1 wherein R may be lower alkyl, aryl, or aralkyl; n may be an integer from 0 to about 10; x may be an integer from 1 to 3; Ar may be substituted or unsubstituted aromatic; R. sub.1 may be lower alkyl, or aralkyl; and pharmaceutically accepted salts thereof. Novel compounds possessing short-acting β-adrenergic blocking activity are also disclosed.
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(2008/06/13)
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