- Catalytic One-Pot Oxetane to Carbamate Conversions: Formal Synthesis of Drug Relevant Molecules
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Oxetanes are versatile building blocks in drug-related synthesis to induce property-modulating effects. Whereas related oxiranes are widely used in coupling chemistry with carbon dioxide (CO2) to afford value-added commodity chemicals, oxetane/CO2couplings remain extremely limited despite the recent advances in the synthesis of these four-membered heterocycles. Here we report an effective one-pot three-component reaction (3CR) strategy for the coupling of (substituted) oxetanes, amines and CO2to afford a variety of functionalized carbamates with excellent chemoselectivity and good yields. The process is mediated by an aluminium-based catalyst under relatively mild conditions and the developed catalytic methodology can be applied to the formal synthesis of two pharmaceutically relevant carbamates with the 3CR being a key step. (Figure presented.).
- Guo, Wusheng,Laserna, Victor,Rintjema, Jeroen,Kleij, Arjan W.
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supporting information
p. 1602 - 1607
(2016/10/13)
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- Carisoprodol method for synthesizing intermediate
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The invention belongs to the field of medicine, and particularly relates to a synthesis method of a carisoprodol intermediate compound, which comprises the following steps: reacting formic acid and isopropylamine to generate N-isopropyl formamide; and adding oxydol into the N-isopropyl formamide, then adding 2-methyl-2-propyl-1,3-propanediol, and reacting to obtain the carisoprodol intermediate compound 2-methyl-2-propyl-3-hydroxypropyl-N-isopropyl carbamate. According to the method, the raw materials are accessible, the reaction process is easy to control, and no serious pollutant is generated in the intermediate process; the stereoselectivity of the reaction is high, and no obvious competing reaction exists; and the method is simple to operate, has specificity and reduces generation of foreign matters, and the product purity is up to 99.5% or above.
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Paragraph 0043; 0044
(2016/10/07)
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- Meprobamate immunoassay
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Carisoprodol is a centrally-acting prescription drug of known abuse. Upon ingestion it is rapidly metabolised to meprobamate, also a prescription drug with abuse potential. Current immunoassays are specific for carisoprodol and therefore have a short window of detection and, furthermore, are ineffective at detecting meprobamate. The current invention, underpinned by an antibody specific for meprobamate, overcomes these deficiencies.
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- CARBAMATE REDUCERS OF SKELETAL MUSCLE TENSION
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The present invention relates to new carbamate skeletal muscle relaxants, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 11
(2010/04/23)
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