专利号:US-5075450-A 优先权日:1990-06-28 标 题 :Intermediates in the synthesis of 17β-acyl-3-carboxy-androsta-3,5-dienes 发明人:RASMUSSON GARY H; TOLMAN RICHARD L; PATEL GOOL F 权利人:MERCK & CO INC 摘要:New intermediates in the synthesis of 17β-acyl-3-carboxy-androsta-3,5-dienes, of the formula: ##STR1## wherein R 2 is 2-thiopyridyl, and n R 3 is C 2 -C 4 alkoxycarbonyl, C 1 -C 4 , or trifluoromethylsulfonyloxy. The above compounds are useful intermediates in producing testosterone 5α-reductase inhibitors which are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
专利号:US-12441733-B2 优先权日:2018-03-26 标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors 发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS 权利人:NOVARTIS AG 摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.
专利号:WO-2012152438-A1 优先权日:2011-05-11 标题 :Process for the preparation of nitrate acid ester of organic compounds 发明人:BONFANTI ANNALISA; STORONI LAURA; RONSIN GAEL 权利人:NICOX SA; BONFANTI ANNALISA; STORONI LAURA; RONSIN GAEL 摘要:The present invention relates to a one-step process for the synthesis of nitric acid esters or 15 N isotopically labeled nitrate esters of organic compounds starting from the correspondent alcohols. Formula (I).
专利号:WO-2023122754-A1 优先权日:2021-12-23 标 题 :Processes and intermediates for preparing gb13, gb22 and himgaline 发明人:LANDWEHR ELEANOR; SHENVI RYAN; BAKER MEGHAN; OGUMA TAKUYA 权利人:SCRIPPS RESEARCH INST 摘要:Provided herein are processes for the streamlined synthesis of Galbulimima alkaloids, such as himbadine, isolated from Galbulimima belgraveana and G. baccatta, trees endemic to the rainforests of Northern Australia and Papua New Guinea, as well as analogs thereof, such as GB13, GB16, GB22, and himgaline, and further including intermediates useful in the synthesis of these and related compounds.
专利号:US-8513465-B2 优先权日:2008-02-04 标题:Potassium organotrifluoroborate derivative and a production method therefor 发明人:KANG HEONJOONG; HAM JUNGYEOB; AHN HONG RYUL; PARK YOUNG HEE 权利人:KANG HEONJOONG; HAM JUNGYEOB; AHN HONG RYUL; PARK YOUNG HEE; SNU R&DB FOUNDATION 摘要:Provided are a production method for a potassium organotrifluoroborate compound having a hydroxyl group, and a novel potassium organotrifluoroborate compound having a hydroxyl group. The production method is advantageous in that a potassium organotrifluoroborate compound can be produced in a single reaction without recourse to a process of isolating and purifying an intermediate. The novel potassium organotrifluoroborate compound having a hydroxyl group is useful as a reactant which is widely used in the total synthesis of physiologically active natural products and diverse organic synthesis reactions including halogen substitution reactions, 1,2- and 1,4-addition reactions using a rhodium (Rh) catalyst, and Suzuki coupling reactions using a palladium (Pd) catalyst.
专利号:US-2004053999-A1 优先权日:1997-09-17 标题 :Novel compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
[参考文献]: B Latli, Et Al. Insecticidal Quinazoline Derivatives With (Trifluoromethyl)Diazirinyl And Azido Substituents As Nadh:Ubiquinone Oxidoreductase Inhibitors And Candidate Photoaffinity Probes. Chem Res Toxicol. 1996 Mar;9(2):445-50.
合成参考文献
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