CAS: 758-08-7; 2-Mercaptoacetamide

上下游产品

2-methoxyethyl 2-mercaptoacetate Methyl thioglycolate ethyl 2-sulfanylacetate Chloroacetamide 4,5,6,7-tetrahydro-cyclopenta[1,4]thiazin-3-one 2,2-diphenyl-thiazolidin-4-one [(4-amino-phenyl)-arsanediyldimercapto]-di-acetic acid diamide 4-oxothiazolidine

📜巯基乙酸甲酯置于氨体系中,用 甲醇 作为反应溶剂,化学反应 14.0H,以100%的收率获得产物2-巯基乙胺
参考文献:一种用碳 14 和氘标记的有效 IKb 激酶-β 抑制剂
标题:一种用碳 14 和氘标记的有效 IKb 激酶-β 抑制剂
摘要:3-氨基-4-(1,1-二氟-丙基)-6-(4-甲磺酰基-哌啶-1-基)-噻吩并[2,3-B]吡啶-2-羧酸酰胺(1)是有效的 IKb 激酶-β (Ikk-β) 抑制剂.描述了这种用碳 14 和氘标记的化合物的有效制备.碳 14 的合成在六个放射化学步骤中完成,总产率为 25%.关键的转化是 2-氰基-(14) C-乙酰胺和酮酯的改良 Guareschi-Thorpe 缩合,然后在一锅中氯化成 2,6-二氯吡啶衍生物.然后将分离的二氯吡啶在一锅中分三步转化为[(14)C]-(1).以54.3 Mci/mmol的比活度和99.8%的放射化学纯度分离出碳14标记(1).使用 4-羟基哌啶-2,2,3,3,4,5,5,6,6-(2) H9 分八步获得标记为 (1) 的氘,总化学产率为 57%.该合成的最后三个步骤在一锅中进行.
DOI:10.1002/jlcr.3398

专利信息

专利号:US-7553646-B2
优先权日:2005-07-28
标题 :Microbial sulfoxidation and amidation of benzhdrylsulfanyl carboxylic acids and uses thereof
发明人：OLIVO HORACIO F; OSORIO-LOZADA ANTONIO VICTOR
权利人:UNIV IOWA RES FOUND
摘要:The present invention provides novel methods for the synthesis of racemic and enantiomers of modafinil via microbial oxidation-amidation transformation. The methods include the successive oxidation-amidation of benzhydrylsulfanyl carboxylic acid to produce racemic and enantiomers of modafinil using at least one microorganism of yeast, bacteria, or fungus. Also disclosed are pharmaceutical compositions of racemic and enantiomers of modafinil along with their use in the treatment of diseases, including attention deficit hyperactivity disorder and drug addiction.

专利号:US-8183294-B2
优先权日:2005-03-14
标 题 :Process for enantioselective synthesis of single enantiomers of thio-substituted arylmethanesulfinyl derivatives by asymmetric oxidation
发明人：LOUVET PHILIPPE; SCHWEIZER DOMINIQUE
权利人:LOUVET PHILIPPE; SCHWEIZER DOMINIQUE; Cephelon France
摘要:The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of:n a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I). nn nwherein Ar, Y, R 1 are as defined in claim 1.

专利号:US-7812193-B2
优先权日:2003-09-19
标题:Process for enantioselective synthesis of single enantiomers of modafinil by asymmetric oxidation
发明人：REBIERE FRANCOIS; DURET GERARD; PRAT LAURENCE
权利人:CEPHALON FRANCE
摘要:The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of:n a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I); nn nwherein n, Y, R 1 , R 1a , R 2 and R 2a are as defined herein.

专利号:US-8816050-B2
优先权日:2006-03-22
标题:Method of preparing glycopeptides
发明人：WONG CHI-HUEY; BRIK ASHRAF; YANG YU-YING; FICHT SIMON; PAYNE RICHARD
权利人:WONG CHI-HUEY; BRIK ASHRAF; YANG YU-YING; FICHT SIMON; PAYNE RICHARD; SCRIPPS RESEARCH INST
摘要:A method is provided for the synthesis of glycopeptides using a sugar assisted ligation strategy, wherein an N-terminal peptide portion in the form of a thioester is coopled with a C-terminal peptide portion bearing a carbohydrate moiety comprising a thiol group.

专利号:US-8759583-B2
优先权日:2003-09-19
标题 :Process for enantioselective synthesis of single enantiomers of modafinil by asymmetric oxidation
发明人：COURVOISIER LAURENT; DURET GERARD; GRAF STEPHANIE; PRAT-LACONDEMINE LAURENCE; REBIERE FRANCOIS; SABOURAULT NICOLAS
权利人:CEPHALON FRANCE; TEVA SANTE
摘要:The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of:n a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I). nn n n n n n n n n n n n wherein n, Y, R 1 , R 1a , R 2 and R 2a are as defined in claim 1.

专利号:US-7153933-B2
优先权日:2001-12-07
标 题 :Solid phase method for synthesis peptide-spacer-lipid conjugates, conjugates synthesized thereby and targeted liposomes containing the same
发明人：WU SHIH-KWANG; CHANG TING-GUNG; TSENG CHIN-LU; CHEN LI-JUNG; SHIH KAE-SHYANG
权利人:DEV CENTER BIOTECHNOLOGY
摘要:A solid phase synthesis method for preparing peptide-spacer-lipid conjugates, the peptide-spacer-lipid conjugates synthesized by the method, and liposomes containing the peptide-spacer-lipid conjugates. The present invention provides a convenient solid phase synthesis method for preparing peptide-spacer-lipid conjugates and provides various linkage groups (such as amide group) for conjugating peptide, spacer and lipid, wherein the spacer may comprise PEG. Several advantages can be achieved, such as the synthetic procedure can be simplified, the synthesis process can be set to automation, the purification is easier in each reaction step, and the product losses can be reduced to minimal during synthesis. The present synthesis method is suitable for preparing a wide range of peptide-spacer-lipid conjugates, provides a peptide-spacer-lipid conjugate prepared by the solid phase synthesis method of the present invention, which can be incorporated into a liposome as the targeting moiety for liposomal drug delivery to specific cells, and provides a targeting liposome containing the present peptide-spacer-lipid conjugate.