2,2-二氟-2-(4-甲氧基苯基)乙酸乙酯置于potassium Carbonate,Silver Nitrate,Selectfluor体系中,用 甲醇,水,丙酮 作为反应溶剂,化学反应 3.0H,反应生成 4-三氟甲基苯甲醚 参考文献:Catalytic Decarboxylative Fluorination For The Synthesis Of Tri-And Difluoromethyl Arenes 标题:Catalytic Decarboxylative Fluorination For The Synthesis Of Tri-And Difluoromethyl Arenes 摘要:Treatment Of Readily Available Alpha,Alpha-Difluoro-And Alpha-Fluoroarylacetic Acids With Selecffluor Under Ag(I) Catalysis Led To Decarboxylative Fluorination. This Operationally Simple Reaction Gave Access To Tri-And Difluoromethylarenes Applying A Late-Stage Fluorination Strategy. Translation To [f-18]Labeling Is Demonstrated Using [f-18]Selectfluor Bis(Triflate),A Reagent Affording [f-18]Tri-And [f-18]Difluoromethylarenes Not Within Reach With [f-18]F-2. DOI:10.1021/ol4009377
专利号:US-2016194279-A1 优先权日:2012-12-09 标 题 :One pot process for the conversion of aroyl chlorides to acyl thioureas 发明人:CHEPURI VENKATA RAMANA; BEERAN SENTHILKUMAR 权利人:COUNCIL SCIENT IND RES 摘要:The present invention disclose an improved one pot process for synthesis of acyl thioureas of formula (I), with yield greater than 80%, from aroyl chlorides of formula (I) wherein, R′ is an aryl or a heteroarylene group substituted with one or more groups selected from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino, carboxyl, ester, halogenated hydrocarbon or an aryl or heteroaryl; R″ and R′″ are selected independently from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino or halogenated hydrocarbon.
专利号:US-2023099421-A1 优先权日:2019-12-17 标题 :A new method of 18f labelling and intermediate salts 发明人:YOUNG ROWAN DRURY; MANDAL DIPENDU; GUPTA RICHA; JAISWAL AMIT KUMAR 权利人:NAT UNIV SINGAPORE 摘要:Disclosed herein is a salt of formula I: where R 1 , X, n, R, R 1 , Y, m, p, q, Z and o are as defined herein. Also disclosed herein are methods of using said salts in chemical synthesis, such as to prepare compounds isotopically enriched in 18F for use in PET & imaging, as well as methods to make the compounds of formula I.
专利号:US-12336981-B2 优先权日:2010-09-03 标题 :Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; DRAGOVICH Peter; GOSSELIN FRANCIS; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; ROTH BRUCE; SMITH CHASE C; WANG ZHONGGUO; YUEN PO-WAI; ZHENG XIAOZHANG 权利人:VALO HEALTH INC; GENENTECH INC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
专利号:US-4996314-A 优先权日:1986-03-11 标题 :6-(disubstituted amino)carbapenem compounds 发明人:YOSHIOKA TAKEO; CHIDA NORITAKA; WATANABE AZUMA; FUKAGAWA YASUO; ISHIKURA TOMOYUKI 权利人:SANRAKU INC 摘要:A compound represented by the formula ##STR1## wherein R 1 represents a lower alkyl group or a lower haloalkyl group; R 2 represents a lower alkyl group, a lower haloalkyl group, an aralkyl group, or a group of the formula --COOR 4 or --SO 2 R 5 in which R 4 represents an aralkyl group or a substituted or unsubstituted alkyl group and R 5 represents an alkyl group or a substituted or unsubstituted aryl group; and R 3 represents a hydrogen atom or a carboxyl protecting group which can be easily split off. This compound is useful in the production of a 6-(disubstituted amino)carbapenem-series antibiotic. n The compounds of the formula ##STR2## wherein R 1 and R 2 are as defined above are important intermediates for the synthesis of the compounds of formula (I) and/or the aforesaid di-(substituted amino) carbapenem-series antibiotics.
专利号:US-11279687-B2 优先权日:2010-09-03 标题:Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; YUEN PO-WAI 权利人:VALO HEALTH INC; GENENTECH INC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An embodiment of the invention is the provision of a compound of Formula IIIA.
专利号:US-9676721-B2 优先权日:2010-09-03 标题 :Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG 权利人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
摘要:Oishi, M.; Takikawa, H., Science of Synthesis Knowledge Updates, (2010) 4, 104. 摘要:Champagne, P. A.; Drouin, M.; Paquin, J.-F., Science of Synthesis Knowledge Updates, (2016) 1, 443. 摘要:Martin, A. R., Science of Synthesis: N-Heterocyclic Carbenes in Catalytic Organic Synthesis, (2016) 1, 177. 摘要:Ouyang, Y.; Shou, J.-Y.; Qing, F.-L., Science of Synthesis: Special Topics, (2022) 1, 276. 摘要:Yoshida, T.; Tobisu, M., Science of Synthesis: Special Topics, (2022) 1, 606.