- Simple and easy synthetic method for key intermediate of dorzolamide hydrochloride
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The invention discloses a simple and easy synthetic method for a key intermediate of dorzolamide hydrochloride. The simple and easy synthetic method for the key intermediate of the dorzolamide hydrochloride comprises the following steps: performing an intramolecular ring-closing reaction on a compound II under the action of an acidic catalyst to form an initial product; performing quenching treatment on the initial product, performing extraction, and performing concentration on an organic phase to obtain a crude product; and performing recrystallization on the crude product, performing filtration, and performing drying to obtain the key intermediate of the dorzolamide hydrochloride. The method provided by the invention has the beneficial effects that the synthetic method for the key intermediate of the dorzolamide hydrochloride is relatively simple, the key intermediate is synthesized in one step, the yield of the product compound I is relatively high, and the product purity is relatively high; and compared with a traditional synthetic method, the synthetic method for the key intermediate of the dorzolamide hydrochloride provided by the invention saves raw material costs, has higher purity of the produced product, and improves a utilization rate of the product.
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Page/Page column 5-8
(2019/10/01)
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- Process for obtaining 4-hydroxy-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-7,7-dioxide and its enantiomers, and applications thereof
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The invention relates to a process for obtaining cis-4-hydroxy-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-7,7-dioxide, its enantiomers or mixtures thereof, by reduction of 5,6-dihydro-6-methyl-4H-thieno[2,3-b]thiopyran-4-one-7,7-dioxide with a reducing agent which generates hydride ions. The obtained compounds are useful as intermediates in the synthesis of chiral active ingredients.
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Page/Page column 1
(2009/12/23)
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- β-Butyrolactone as a chiral building block in organic synthesis: A convenient synthesis of MK-0507 keto sulfone
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The nucleophilic ring opening of (R)-β-butyrolactone 2 with 2-thiophenethiolate is the key step in a straightforward stereospecific synthesis of keto sulfone 1, a precursor to carbonic anhydrase inhibitor MK-0507.
- Tempkin, Orin,Blacklock, Thomas J.,Burke, J. Andrew,Anastasia, Maria
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p. 2721 - 2724
(2007/10/03)
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