专利号:US-6048991-A 优先权日:1990-11-16 标题:Preparation of epoxides 发明人:HAERMELING DIETER 权利人:BASF AG 摘要:Alpha-hydroxy-epoxides of alpha-alkoxy-epoxides of the formula IV ##STR1## in which the substituents have the following meanings: R 7 , R 8 , R 9 , R 10 , R 11 are independently hydrogen, C 1 -C 20 -alkyl, C 3 -C 12 -cycloalkyl, C 4 -C 20 -cycloalkylalkyl, C 1 -C 20 -hydroxy-alkyl, a heterocyclic ring, or an aryl or C 7 -C 20 -arylalkyl group optionally substituted by C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, halogen, C 1 -C 4 -haloalkyl, C 1 -C 4 -halo-alkoxy, phenyl, phenoxy, halophenyl, halophenoxy, carboxy, C 2 -C 8 -alkoxycarbonyl, or cyano, or R 7 and R 8 or R 7 and R 9 or R 7 and R 10 or R 9 and R 10 or R 10 and R 11 together form a (CH 2 ) n group in which n is an integer from 1 to 10 and which may be optionally substituted by C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, and/or halogen, and n R 12 is hydrogen, C 1 -C 8 -alkyl, or benzyl, n provided that R 10 is not hydrogen, methyl, ethyl, propyl, or cyclohexyl when R 7 , R 8 , R 9 , or R 11 is hydrogen, that R 7 is not methyl when R 8 is methyl or phenyl and R 9 , R 10 , or R 11 is hydrogen, that R 7 is not methyl when R 8 , R 9 , R 10 , or R 11 is hydrogen and R 12 is ethyl, that R 7 is not phenyl or hexyl when R 8 , R 9 , R 10 , or R 11 is hydrogen, that R 9 is not methyl when R 7 , R 8 , R 10 , or R 11 is hydrogen, that R 10 and R 11 are not methyl when R 7 , R 8 , or R 9 is hydrogen, and that R 7 and R 10 do not together form an unsubstituted cycloalkyl when R 8 , R 9 , or R 11 is hydrogen. The epoxides of the above formula serve as intermediates for the synthesis of, inter alia, perfumes, plant protectants and polymers.
专利号:US-4808607-A 优先权日:1985-05-22 标题 :Imidazole analogs of mevalonolactone and derivatives thereof for use in inhibiting cholesterol biosynthesis and lowering blood cholesterol level 发明人:WAREING JAMES R 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Compounds of the formula and the pharmaceutically acceptable acid addition salts thereof, wherein the various substituents are defined hereinbelow and the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
专利号:US-9803050-B2 优先权日:2014-10-08 标 题:Dispersant for use in synthesis of polyaryletherketones 发明人:NAIR KAMLESH P 权利人:TICONA LLC 摘要:A method for forming a polyaryletherketone is described. More particularly, a reaction mixture is initially supplied to the reactor vessel that contains one or more precursor monomers. A heteroaryl compound is also added to the reaction mixture. The reaction can be carried out according to, e.g., an electrophilic aromatic substitution reaction or a nucleophilic aromatic substitution reaction. The heteroaryl compound can serve as a dispersant to the polymer as it is formed. This minimizes the likelihood of gelling of the product polymer within the reactor vessel and limits the impact of process disruptions on the production of the polyaryletherketone.
专利号:US-11344858-B2 优先权日:2019-05-02 标 题 :Micro-electrolysis reactor for ultra fast, oxidant free, C—C coupling reaction and synthesis of daclatasvir analogs thereof 发明人:SINGH AJAY KUMAR; PABBARAJA SRIHARI; GHOSH SUBHASH; BHUSHAN MAHAJAN; MUJAWAR TAUFIQUEAHMED 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to a continuous micro-electro-flow reactor system for ultra-fast, oxidant free, C—C coupling reaction for making symmetrical biaryls and analogs thereof. This invention further relates to the said process for preparation of antiviral drug, daclatasvir of general formula I.
专利号:US-12364961-B2 优先权日:2021-01-13 标 题 :Multiplex synthesis method of compound library and parallel synthesizer of compound library using same 发明人:KIM DONG PYO; AHN GWANG NOH 权利人:POSTECH RES & BUSINESS DEV FOUND 摘要:The present invention relates to a parallel synthesis method and synthesizer of a compound library, and more specifically provides a parallel synthesis method and synthesizer of a compound library, which uniformly distribute a first reactant and perform independent reactions in separate spaces, and since it is possible to confirm the results for various reaction variables at once, the synthesis time of the compound library can be reduced with a high synthesis yield of the product.
专利号:WO-2024258613-A9 优先权日:2023-06-16 标题:Tetrachlorovancomycin and derivatives 发明人:BOGER DALE 权利人:SCRIPPS RESEARCH INST 摘要:A total synthesis of a new class of vancomycin analogues of reduced synthetic complexity was developed. The synthesis, achieved by the addition of two aryl chloride substituents to provide tetrachlorovancomcyin aglycon (Compound II), tetrachlorovancomcyin (Compound I ), and their derivatives, permitted a streamlined total synthesis of the new class of glycopeptide antibiotics by removing atropisomer stereochemical control and enabled the simultaneous and further activated SNAr macrocyclizations that establish the tricyclic skeleton of Compound I. In addition to the antimicrobial evaluation of tetrachlorovancomycin (Compound I), the preparation of key binding pocket and peripherally-modi fied derivatives, which overcome vancomycin resistance and introduce independent and synergistic mechanisms of action, revealed their exceptional antimicrobial potency and provide the foundation for use of this new class of synthetic glycopeptide analogues. Also disclosed are a pharmaceutical composition containing bactericidal amount of tetrachlorovancomycin, a derivative thereof or a salt of either dissolved or dispersed in a pharmaceutically acceptable diluent.
摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 594. 摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 571. 摘要:Amatore, M.; Aubert, C.; Malacria, M.; Petit, M., Science of Synthesis Knowledge Updates, (2012) 3, 99. 摘要:Hall, D. G.; Zheng, H., Science of Synthesis Knowledge Updates, (2011) 4, 99. 摘要:Spivey, A. C.; Tseng, C.-C., Science of Synthesis Knowledge Updates, (2010) 1, 44.