- Method for synthesizing chloroformate compound through continuous flow
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The invention provides a method for synthesizing a chloroformate compound through continuous flow, and belongs to the field of synthesis processes. The method comprises the following steps: taking a compound X and triphosgene as raw materials, and reacting in a continuous flow reactor under the action of a catalyst to obtain the chloroformate compound, wherein the structure of the compound X is the structure of a chloroformate compound. The efficient and green preparation of the chloroformate compound is realized by utilizing the continuous flow synthesis method disclosed by the invention. In addition, the continuous flow synthesis method disclosed by the invention obviously shortens the reaction time, solves the instability factor of using phosgene in the amplified production process, and is more beneficial to industrial amplified production.
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Paragraph 0063-0074
(2022/01/10)
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- Design and Comparative Evaluation of the Anticonvulsant Profile, Carbonic-Anhydrate Inhibition and Teratogenicity of Novel Carbamate Derivatives of Branched Aliphatic Carboxylic Acids with 4-Aminobenzensulfonamide
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Epilepsy is one of the most common neurological diseases, with between 34 and 76 per 100,000 people developing epilepsy annually. Epilepsy therapy for the past 100+ years is based on the use of antiepileptic drugs (AEDs). Despite the availability of more than twenty old and new AEDs, approximately 30% of patients with epilepsy are not seizure-free with the existing medications. In addition, the clinical use of the existing AEDs is restricted by their side-effects, including the teratogenicity associated with valproic acid that restricts its use in women of child-bearing age. Thus, there is an unmet clinical need to develop new, effective AEDs. In the present study, a novel class of carbamates incorporating phenethyl or branched aliphatic chains with 6–9 carbons in their side-chain, and 4-benzenesulfonamide-carbamate moieties were synthesized and evaluated for their anticonvulsant activity, teratogenicity and carbonic anhydrase (CA) inhibition. Three of the ten newly synthesized carbamates showed anticonvulsant activity in the maximal-electroshock (MES) and 6?Hz tests in rodents. In mice, 3-methyl-2-propylpentyl(4-sulfamoylphenyl)carbamate(1), 3-methyl-pentan-2-yl-(4-sulfamoylphenyl)carbamate (9) and 3-methylpentyl, (4-sulfamoylphenyl)carbamate (10) had ED50 values of 136, 31 and 14?mg/kg (MES) and 74, 53, and 80?mg/kg (6?Hz), respectively. Compound (10) had rat-MES-ED50 = 13?mg/kg and ED50 of 59?mg/kg at the mouse-corneal-kindling test. These potent carbamates (1,9,10) induced neural tube defects only at doses markedly exceeding their anticonvuslnat-ED50 values. None of these compounds were potent inhibitors of CA IV, but inhibited CA isoforms I, II and VII. The anticonvulsant properties of these compounds and particularly compound 10 make them potential candidates for further evaluation and development as new AEDs.
- Bibi, David,Mawasi, Hafiz,Nocentini, Alessio,Supuran, Claudiu T.,Wlodarczyk, Bogdan,Finnell, Richard H.,Bialer, Meir
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p. 1972 - 1982
(2017/07/17)
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- Identification, synthesis, and strategy for the reduction of potential impurities observed in dabigatran etexilate mesylate processes
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Synthetic impurities that are present in dabigatran etexilate mesylate were studied, and possible pathways by which these impurities are formed during the manufacturing process were examined. The impurities were monitored by high-performance liquid chromatography, and their structures were determined by mass spectrometry and 1H and 13C NMR. Potential causes for the formation of these impurities are discussed, and strategies to minimize their formation are also described.
- Zheng, Yong-Yong,Shen, Cheng-Wu,Zhu, Mei-Yu,Zhou, Yi-Meng,Li, Jian-Qi
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p. 744 - 750
(2014/07/08)
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- 1-(N-Octylthiocarbonyl)-2-(4-thiazolyl)benzimidazole
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New benzimidazoles substituted at the 1-position with carbonyl substituents and at the 2-position with a 4-thiazolyl group are effective fungicides and anthelmintics. The compounds as well as processes for their preparation are described along with antifungal and anthelmintic compositions for their use. The 1-position substituent is a hydrocarbon group of from 5 to 12 carbon atoms connected to the carbonyl group through an oxygen or a sulfur atom. The compounds are generally prepared by contacting a 1-unsubstituted benzimidazole with a hydrocarbon radical substituted chloroformate or chlorothiol formate.
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