- Mechanochemical Synthesis of Primary Amides
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Ball milling of aromatic, heteroaromatic, vinylic, and aliphatic esters with ethanol and calcium nitride afforded the corresponding primary amides in a transformation that was compatible with a variety of functional groups and maintained the integrity of a stereocenter α to carbonyl. This methodology was applied to α-amino esters and N-BOC dipeptide esters and also to the synthesis of rufinamide, an antiepileptic drug.
- Gómez-Carpintero, Jorge,Sánchez, J. Domingo,González, J. Francisco,Menéndez, J. Carlos
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p. 14232 - 14237
(2021/10/20)
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- Synthesis method of 2-formyl-4-carboxylic acid ethyl thiazole
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The invention discloses a synthesis method of 2-formyl-4-carboxylic acid ethyl ester thiazole, the synthesis method takes dichloroacetic acid, sodium ethoxide and ethanol as initial raw materials to firstly synthesize 2,2-diethoxyacetic acid ethyl ester, then ammonia water is added to ammoniate to obtain 2,2-diethoxyacetamide, the 2,2-diethoxyacetamide is converted into 2,2-diethoxythioacetamide through thioation by use of a vulcanizing reagent, then the 2,2-diethoxythioacetamide is condensed with 3-ethyl bromopyruvate to generate 2-diethoxymethyl-4-carboxylic acid ethyl ester thiazole, and finally acid deprotection is performed in an acetone solution to obtain the 2-formyl-4-carboxylic acid ethyl ester thiazole. According to the synthesis method of the 2-formyl-4-carboxylic acid ethyl ester thiazole, and the used raw materials are low in price, high in safety and easy to obtain. In addition, the synthesis method has the advantages of short synthesis route, high yield, high chemical purity of the obtained product, no need of complicated operation, and large-scale production.
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Paragraph 0017; 0019; 0025; 0029; 0031; 0035; 0037; 0041
(2019/11/18)
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- NOVEL MINOR GROOVE BINDERS
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There is provided compounds of formula (I), wherein R1, R11, R12, Qa, X, Qb, Qc, A and D have meanings given in the description, or a pharmaceutically acceptable salt or solvate thereof, which compound, salt or solvate binds to the minor groove of DNA.
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Page/Page column 3
(2008/06/13)
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- A formal synthesis of althiomycin
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A formal synthesis of the antibiotic althiomycin has been completed preliminary to studies of the interaction of this compound with prokaryotic ribosomes.
- Toogood, Peter L.,Hollenbeck, Jessica J.,Lam, Huong M.,Li, Li
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p. 1543 - 1546
(2007/10/03)
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