CAS: 690662-96-5; (3-(Piperidin-1-Ylsulfonyl)Phenyl)Boronic Acid

📜3-(6-Methyl-[1,3,6,2]Dioxazaborocan-2-yl)-Benzenesulfonyl Chloride置于dowex 50Wx2-400 Resin体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 3-(哌啶-1-基磺酰)苯基硼酸
参考文献:Synthesis Of Sulfonyl Chlorides Of Phenylboronic Acids
标题:Synthesis Of Sulfonyl Chlorides Of Phenylboronic Acids
摘要:苯基硼酸酯的磺酰氯可通过选择性锂化溴代n-甲基二乙醇胺苯基硼酸盐,反应生成锂亚磺酰苯基硼酸盐中间体,再通过与n-氯代琥珀酰亚胺氧化,得到目标磺酰氯.这些新的试剂在制备苯基硼酸的磺酰胺以及其他化合物中非常有用,这些化合物可用于钯(0)催化的交叉偶联反应.此外,它们还具有作为生理pka条件下碳水化合物结合剂的潜力.
DOI:10.1055/s-2004-817758

专利信息

专利号:US-6872849-B2
优先权日:2002-11-08
标题 :Halo sulfonyl aryl boronates
发明人：VEDSO PER; OLESEN PREBEN HOULBERG; HOEG-JENSEN THOMAS
权利人:NOVO NORDISK AS
摘要:The present invention relates to halo sulfonyl aryl boronates of the general formula (I): n n wherein Arylene designates a carbocyclic or heterocyclic, aromatic ring system comprising 1-3 rings; R 1 , R 2 and R 3 are, independently, hydrogen, C 1-6 alkyl, C 1-6 alkoxy, halogen, nitro, cyano or phenyl; X is fluoro, chloro or bromo; and Y is a boroxine moiety attached via a bond from Arylene to one of the boron atoms of a boroxine ring which ring has a group of the formula -Arylene(R 1 )(R 2 )(R 3 )SO 2 X, wherein Arylene, R 1 , R 2 , R 3 and X are as defined above, at each of the other two boron atoms of the boroxine ring, or Y is a boronic acid group or a boronic ester group. The invention also relates to the preparation of the compounds of formula (I) and to their use in organic synthesis.

专利号:EP-1562961-B1
优先权日:2002-11-08
标 题 :Halo sulfonyl aryl boronates
发明人：VEDSO PER; OLESEN PREBEN HOULBERG; HOEG-JENSEN THOMAS
权利人:NOVO NORDISK AS
摘要:The present invention relates to halo sulfonyl aryl boronates of the general formula (I): wherein Arylene designates a carbocyclic or heterocyclic, aromatic ring system comprising 1-3 rings; R<1>, R<2> and R<3> are, independently, hydrogen, C1-6alkyl, C1-6alkoxy, halogen, nitro, cyano or phenyl;X is fluoro, chloro or bromo; and Y is a boroxine moiety attached via a bond from Arylene to one of the boron atoms of a boroxine ring which ring has a group of the formula -Arylene(R<1>)(R<2>)(R<3>)SO2X, wherein Arylene, R<1>, R<2>, R<3> and X are as defined above, at each of the other two boron atoms of the boroxine ring, or Y is a boronic acid group or a boronic ester group.The invention also relates to the preparation of the compounds of formula (I) and to their use in organic synthesis.