磺酸己烷置于磺酰氯体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 3.0H,反应生成2-己基磺酰氯 参考文献:Rearrangement Of Sulfonamidyl Radicals With Hydrogen Migration 标题:Rearrangement Of Sulfonamidyl Radicals With Hydrogen Migration 摘要: Doi:10.1007/bf00954818
专利号:US-6639059-B1 优先权日:1999-03-24 标 题 :Synthesis of [2.2.1]bicyclo nucleosides 发明人:KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M 权利人:EXIQON AS 摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs.
专利号:US-6734291-B2 优先权日:1999-03-24 标题:Synthesis of [2.2.1]bicyclo nucleosides 发明人:KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M 权利人:EXIQON AS 摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs
专利号:US-6228988-B1 优先权日:1995-02-24 标题:Synthesis of hydroxamic acid derivatives 发明人:FLOYD CHRISTOPHER DAVID; LEWIS CHRISTOPHER NORMAN 权利人:BRITISH BIOTECH PHARM 摘要:The present invention describes processes for preparing desired synthetic products that comprise a covalently bonded hydroxamic acid group -CONHOH by forming a mixture of a liquid reaction medium and a solid phase reaction product that carries a plurality of moieties of formula (A1) or (B1):where X is a residual, non-hydroxamate partial structure of the desired synthetic product, P1 is hydrogen or an amino-protecting group, P2 is hydrogen or a hydroxyl protecting group, and the bond designated (a) covalently links the moieties (A1) or (B1) to the residue of a solid substrate; by cleaving the bond designated (a) in the resultant mixture; and by separating the resultant liquid reaction phase from the resultant reaction solids to recover the desired synthetic product.
专利号:US-8138272-B2 优先权日:2006-05-22 标 题:Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds 发明人:KONRADI ANDREI W; SMITH JENIFER L 权利人:KONRADI ANDREI W; SMITH JENIFER L; ELAN PHARM INC 摘要:This invention provides an improved synthesis of polymer conjugates of formula (I), n nof agricultural, therapeutic, and food additive compounds. In particular, a process is described for the preparation of conjugates by treating primary or secondary alcohol substituents of active compounds with polymeric nucleophiles using “Mitsunobuâ€? or related reaction conditions.
专利号:US-2003092905-A1 优先权日:1999-03-24 标 题:Synthesis of [2.2.1]bicyclo nucleosides
专利号:US-6093798-A 优先权日:1995-02-24 标题 :Synthesis of hydroxamic acid derivatives
参考标题:Clean And Economic Synthesis Of Alkanesulfonyl Chlorides From S-Alkyl Isothiourea Salts Via Bleach Oxidative Chlorosulfonation 作者:Jiaxi Xu,Zhanhui Yang,Bingnan Zhou 摘要:Abstract A Simple Procedure For Clean And Economic Synthesis Of Alkanesulfonyl Chlorides Via Bleach-Mediated Oxidative Chlorosulfonation Of S-Alkyl Isothiourea Salts Is Disclosed. This Procedure Is Environment- And Worker-Friendly With The Advantages Of Readily Accessible Materials And Reagents, Simple And Safe Operations, Easy Purification Without Chromatography, And Affords High Yields Of Up To 99%
合成参考文献
摘要:Drabowicz, J.; Kiełbasiński, P.; Łyżwa, P.; Zając, A.; Mikołajczyk, M., Science of Synthesis, (2008) 39, 33.