专利号:US-11220513-B2 优先权日:2015-04-30 标题:Chromium-mediated coupling and application to the synthesis of halichondrins 发明人:KISHI YOSHITO; YAN WUMING; LI JINGWEI; LI ZHANJIE; YAHATA KENZO 权利人:HARVARD COLLEGE 摘要:The present invention provides unified synthesis of the C1-C19 building blocks of halichondrins and analogs thereof using selective coupling of poly-halogenated nucleophiles in chromium-mediated coupling reactions. The present invention also provides a practical and efficient synthesis of C20-C38 building blocks of halichondrins and analogs thereof. Also provided herein are general methods of selective activation and coupling of poly-halogenated analogs with an aldehyde. The provided coupling reactions are selective for halo-enone and halo-acetylenic ketal over vinyl halide and halide attached to a sp hybridized carbon. The provided efficient selective coupling reactions can allow easy access to the C1-C19 building blocks and C20-C38 building blocks of halichondrins and analogs thereof with limited or no purification or separation of the intermediates.
专利号:US-7718578-B2 优先权日:2003-03-31 标 题 :Method of synthesis and testing of combinatorial libraries using microcapsules 发明人:GRIFFITHS ANDREW DAVID; ABELL CHRIS; HOLLFELDER FLORIAN; MASTROBATTISTA ENRICO 权利人:MEDICAL RES COUNCIL 摘要:The invention describes a method for the synthesis of compounds comprising the steps of: (a) compartmentalizing two or more sets of primary compounds into microcapsules; such that a proportion of the microcapsules contains two or more compounds; and (b) forming secondary compounds in the microcapsules by chemical reactions between primary compounds from different sets. The invention further allows for the identification of compounds which bind to a target component of a biochemical system or modulate the activity of the target, and which is co-compartmentalized into the microcapsules.
专利号:US-8901304-B1 优先权日:2013-11-05 标题:Benzo[D]imidazole derivatives of piperidine and piperazine 发明人:ULLAH NISAR 权利人:UNIV KING FAHD PET & MINERALS; KING ABDULAZIZ CITY SCI & TECH 摘要:The benzo[d]imidazole derivatives of piperidine and piperazine are 5-piperazinyl and 5-piperadinyl-1H-benzo[d]imidazol-2(3H)-ones that exhibit D 2 and 5-HT 1A receptor binding affinities, making them suitable for use as the active ingredient of pharmaceuticals for the treatment of schizophrenia. The derivatives have the general formula: n nwhere X is carbon or nitrogen and R is a selected biaryl group, or a pharmaceutically acceptable salt thereof. The piperidinyl compounds are prepared by removal of the Boc group from tert-Butyl-4-(2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)piperidine-1-carboxylate. Subsequent reductive amination with a selected biarylaldehyde completes the synthesis of the 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones. The piperazinyl compounds are prepared by preparation of the intermediate tert-Butyl 4-(3,4-diaminophenyl)piperazine-1-carboxylate. Removal of the Boc group and subsequent reductive amination with a selected biarylaldehyde completes the synthesis of the 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.
专利号:RU-2035448-C1 优先权日:1992-04-20 标题:2-acetonyl-5,5-dimethyl-1,2,3,4,5,6,7,8-octahydronaphthalene as a component of perfumery composition, method of its synthesis, 2,6-dimethyl-2,6,10-tridecatriene-12-one as an intermediate product in synthesis of 2-acetonyl-5,5-dimethyl-1,2,3,4,5,6,7,8-octahydronaphthalene
专利号:US-7501536-B2 优先权日:2005-01-19 标题 :Odorant compounds, synthesis method, and uses of said compounds 发明人:JAUNKY PIOTR; MANE JEAN; SCHROEDER MARTIN 权利人:MANE FILS V 摘要:A compound of general formula (I) with or without the double bond illustrated by the dotted line. In formula (I), X is a CHO, CH2OH, CH2OC(O)R or CH(OR)2 group, and R represents a linear or branched C1-C5 alkyl or alkenyl chain. The synthesis method for the compound, and especially the 6,8-dimethyl-non-7-enal (1) prepared by the hydroformylation of the 5,7-dimethyl-octa-1,6-diene is also disclosed, as well as compositions containing the compounds of formula (I). Due to the odorant properties thereof, the compounds are highly useful in perfumery, especially for cosmetic products and household products.
专利号:US-9925504-B2 优先权日:2004-03-31 标 题 :Compartmentalised combinatorial chemistry by microfluidic control 发明人:GRIFFITHS ANDREW; WEITZ DAVID; AHN KEUNHO; LINK DARREN; BIBETTE JEROME 权利人:GRIFFITHS ANDREW; WEITZ DAVID; AHN KEUNHO; LINK DARREN; BIBETTE JEROME; HARVARD COLLEGE; MEDICAL RES COUNCIL 摘要:The invention describes a method for the synthesis of compounds comprising the steps of: (a) compartmentalizing two or more sets of primary compounds into microcapsules; such that a proportion of the microcapsules contains two or more compounds; and (b) forming secondary compounds in the microcapsules by chemical reactions between primary compounds from different sets; wherein one or both of steps (a) and (b) is performed under microfluidic control; preferably electronic microfluidic control The invention further allows for the identification of compounds which bind to a target component of a biochemical system or modulate the activity of the target, and which is co-compartmentalized into the microcapsules.
摘要:Rueda-Becerril, M.; Sammis, G. M., Science of Synthesis Knowledge Updates, (2017) 2, 215. 摘要:Jie, X.; Su, W., Science of Synthesis, (2022) , 36. 摘要:Chen, P.; Liu, G., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 231. 摘要:Food and Cosmetics Toxicology., 2(327), 1964 摘要:S13 | EUCOSMETICS | Combined Inventory of Ingredients Employed in Cosmetic Products (2000) and Revised Inventory (2006) | DOI:10.5281/zenodo.2624118