专利号:WO-2025030970-A1 优先权日:2023-08-04 标 题:Condensing agent and use thereof in preparation of isothiocyanate 发明人:SI XIAOJIA; CHEN QUAN; LEI AIWEN; YI HONG; CHEN YI-HUNG 权利人:HUAWEI TECH CO LTD 摘要:The present application relates to the field of organic synthesis. Provided is a condensing agent. The condensing agent has formula 1, wherein R1 and R2 are each independently selected from the same or different electron-withdrawing groups. Compared with thiophosgene or carbon disulfide used in a traditional solution, the condensing agent provided in the embodiments of the present application has lower toxicity, and the condensing agent is a solid, such that the diffusion of pollution is easily controlled. Therefore, the condensing agent provided in the embodiments of the present application can be used for environmentally friendly synthesis of an isothiocyanate compound and has relatively small influence on the environment. Moreover, the condensing agent provided in the embodiments of the present application comprises electron-withdrawing groups, such that the yield of the isothiocyanate compound can be increased.
专利号:US-2023046065-A1 优先权日:2019-11-25 标题 :MERGING C(sp3)-H ACTIVATION WITH DNA-ENCODING 发明人:YU JIN-QUAN 权利人:SCRIPPS RESEARCH INST 摘要:Palladium-catalyzed C(sp3)—H arylation of aliphatic carboxylic acids, amides and ketones with BNA-encoded aryl iodides in water is disclosed, Furthermore, sequential C—H arylation chemistry enabled the on-DNA synthesis of structurally-diverse scaffolds containing enriched C(sp3) character, chiral centers, cyclopropane, cyclobutane, and heterocycles. That new chemistry permits preparation of a DNA—encoded library (BEL) technology that can dramatically expedite hit identification in drug discovery owing to its ability to perform protein affinity selection with millions or billions of molecules in a single experiment. The sequential functionalization of multiple C—H bonds provides an unique avenue for creating diversity and complexity from simple starting materials. The use of water as solvent, the presence of DMA, and the extremely low concentration of DMA-encoded coupling partners (0.001 M) have previously hampered the development DMA-encoded C(sp3)—H activation reactions, but many of those hurdles have now been overcome.
专利号:US-3963734-A 优先权日:1971-09-17 标 题:Lower alkylsulfonyl 2-amino, 3-nitro pyridines 发明人:DOHERTY GEORGE O P; FUHR KENNETH H 权利人:LILLY CO ELI 摘要:Substituted 1-hydroxy-2-(1,1-difluoroalkyl)-1H-imidazo-(4,5-b)pyridine compounds useful as herbicides; and intermediates useful in the synthesis of these compounds. In addition to exhibiting herbicidal activity, the substituted 1-hydroxy-2-(1,1-difluoroalkyl)-1H-imidazo(4,5-b)pyridine compounds are of low mammalian toxicity.
专利号:US-4087432-A 优先权日:1974-05-23 标 题 :1H-imidazo(4,5-b)pyridine compounds 发明人:O DOHERTY GEORGE O P; FUHR KENNETH H 权利人:LILLY CO ELI 摘要:Substituted 1-hydroxy-2-(1,1-difluoroalkyl)-1H-imidazo-(4,5-b)pyridine compounds useful as herbicides; and intermediates useful in the synthesis of these compounds. In addition to exhibiting herbicidal activity, the substituted 1-hydroxy-2-(1,1-difluoroalkyl)-1H-imidazo(4,5-b)pyridine compounds are of low mammalian toxicity.
专利号:US-3968116-A 优先权日:1971-09-17 标 题 :1H-imidazo(4,5-b)pyridine compounds 发明人:DOHERTY GEORGE O P; FUHR KENNETH H 权利人:LILLY CO ELI 摘要:Substituted 1-hydroxy-2-(1,1-difluoroalkyl)-1H-imidazo-(4,5-b)pyridine compounds useful as herbicides; and intermediates useful in the synthesis of these compounds. In addition to exhibiting herbicidal activity, the substituted 1-hydroxy-2-(1,1-difluoroalkyl-1H-imidazo(4,5-b)pyridine compounds are of low mammalian toxicity.
专利号:WO-2023168649-A1 优先权日:2022-03-10 标 题 :Method for preparing mefunidone hydrochloride 发明人:WANG XINGWANG; LIN ZHAIWEI; ZHENG QINXIANG 权利人:GUANGZHOU NUCIEN PHARMACEUTICAL CO LTD 摘要:The present invention relates to a method for preparing mefunidone hydrochloride. Compared with the prior art, one synthesis step is omitted, and the yield is improved, wherein the yield of step 3 in the present invention is 90.0%, and the yield of the finished product ZHC-114 is improved by 10%. The present invention further avoids the use of hydrochloric acid, which is more corrosive than HCO 2 H. In addition, due to the improvement in yield, the overall production cost is reduced, the use of hydrochloric acid is avoided, and the environmental protection cost is also reduced.
[参考文献]: Nora Badawi, Et Al. Environmental Fate Of The Herbicide Fluazifop-P-Butyl And Its Degradation Products In Two Loamy Agricultural Soils: A Combined Laboratory And Field Study. Environ Sci Technol. 2015 Aug 4;49(15):8995-9003.