63659-17-6Relevant articles and documents
PROCESS FOR PREPARATION OF PHENOXYPROPANOL AMINES
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Page/Page column 8-9, (2010/04/06)
The present invention describes an improved method for the preparation of l-[4-{2- (cyclopropylmethoxy)ethyl}phenoxy]-3-[(1-methylethyl)amino]-2-propanol of Formula-(I) and its pharmaceutically acceptable salt, which comprises reacting 4 - [ 2 — (Cyclopropylmethoxy) ethyl] phenol with epichlorohydrin in presence of mild base and polar protic solvent to isolate 1 - {4 - [2 - (cyclopropylmethoxy)ethyl] - phenoxy} - 2, 3 - epoxy propane, which is further reacted with isopropyl amine to get betaxolol formula (I).
Process for the selective alkylation of betaxolol intermediates
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, (2008/06/13)
The present invention relates to a process for the selective alkylation of intermediates of betaxolol.
Design and synthesis of a series of combined vasodilator/β-adrenoceptor antagonists based on 6-arylpyridazinones
Slater,Howson,Swayne,Taylor,Reavill
, p. 345 - 351 (2007/10/02)
A series of new 6-[4-[[(aryloxy)acyl]amino]phenyl]-4,5-dihydropyridazinones have been synthesized and evaluated as combined vasodilator/β-adrenoceptor antagonists and potential antihypertensive agents. Many of the early compounds displayed an unacceptably high level of intrinsic sympathomimetic activity (ISA) and a relatively short duration of action. Disubstitution in the 2,3-positions or in the 4-position of the aryloxy ring gave compounds with low ISA levels and, in some instances, improved duration of action. All of the compounds were vasodilators, but the 5-methylpyridazinone derivatives showed consistently greater antihypertensive activity than their 5-H lower homologues. Further detailed pharmacological investigations led to the selection of 6-[4-[3-[[2-hydroxy-3-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]propyl]amino ]propionamido]phenyl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone (4t) (SK&F 95018) as a development candidate.