- Substituted aromatic amino-alcohol compound, and preparation method and application thereof
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The invention relates to a compound of a formula (I) or pharmaceutically acceptable salts thereof. In the formula (I), Ar is an aryl, a heteroaryl or the aryl or the heteroaryl which is substituted byone or more of C1-C6 alkyl, halogen, hydroxyl, amido, sulfydryl, aryl or heterocyclyl; X is O, NH or S; R is C1-C4 fatty alkyl or the C1-C4 fatty alkyl which is substituted by halogen or phenyl; n equals to 1 to 3. The invention also provides a preparation method and application of the compound of the formula (I) or the pharmaceutically acceptable salts thereof. The compound provided by the invention can be used for treatment of hemangiomas or vascular malformations. (The formula (I) is shown in the description).
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Paragraph 0127-0131
(2019/01/05)
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- Enantioselective synthesis of (S)-timolol via kinetic resolution of terminal epoxides and dihydroxylation of allylamines
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An efficient enantioselective synthesis of (S)-timolol has been described using chiral Co-salen-catalyzed kinetic resolution of less expensive (±)-epichlorohydrin with 3-hydroxy-4-(N-morpholino)-1,2,5-thiadiazole in good overall yield (55%) and excellent enantioselectivity (98%). Synthesis of (S)-timolol has also been achieved using hydrolytic kinetic resolution as well as asymmetric dihydroxylation routes in 90% ee and 56% ee, respectively.
- Narina, Srinivasarao V.,Sudalai, Arumugam
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p. 3026 - 3030
(2007/10/03)
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- Novel methods and compounds employed therein
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Preparation of an optically active alkamine in the sinister configuration, or a derivative of said alkamine, which is reacted with an 3-X-4-chloro(or RO-- where R is hydrogen or an alkali metal)-1,2,5-thiadiazole to prepare S-3-X-4-(3-substituted amino-2-hydroxypropoxy)-1,2,5-thiadiazole beta adrenergic blocking agents. Novel 3-morpholino-4-chloro(or RO--)-1,2,5-thiadiazoles and their preparation also are described.
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