CAS: 68524-30-1; 2-[(Diphenylmethyl)Thio]Acetamide

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CAS号90-99-3 二苯基氯甲烷 | CAS号79-07-2 氯乙酰胺 | CAS号121-44-8 三乙胺 | CAS号68524-29-8 2-benzhydrylsul... | CAS号63547-22-8 2-[(二苯甲基)巯基]乙酸 | CAS号118286-24-1 methyl diphenyl... | CAS号4237-48-3 二苯基硫代甲烷 | CAS号90280-15-2 benzhydrylsulfa... | CAS号683-57-8 2-溴乙酰胺 | CAS号91-01-0 二苯甲醇 | CAS号112111-43-0 莫达非尼 | CAS号63547-24-0 2-二苯基甲基亚砜基乙酸 | CAS号6266-48-4 2,4,6-tribenzhy...

Benzhydrylsulfanyl Acetyl Chloride置于ammonium Hydroxide体系中,用 水 作为反应溶剂,化学反应 20.0H,反应生成 二苯甲基硫代乙酰胺
参考文献:甲酰胺催化的羧酸活化--通用且经济高效的酰胺化和酯化†
标题:甲酰胺催化的羧酸活化--通用且经济高效的酰胺化和酯化†
摘要:基于甲酰基吡咯烷 (Fpyr) 作为路易斯碱催化剂,提出了一种新的,广泛适用的酰胺 C-N 和酯 C-O 键形成方法.在此,三氯三嗪 (Tct) 是用于 Oh 基团活化的最具成本效益的试剂,其用量相对于起始材料 (100 Mol%) <=40 Mol%.新方法的特点是卓越的成本效益,废物平衡(e-因子降至 3)和可扩展性(高达 >80 G).此外,还证明了高水平的官能团相容性,包括酸不稳定的缩醛和甲硅烷基醚,甚至可以形成肽 C-N 键.与使用 Tct 的报道酰胺化过程相比,产率显着提高(例如从 26% 到 91%),并且酯化首次在合成有用的产率中得到促进.这些显着的改进通过使用酰氯而不是较少亲电子酸酐中间体的活化来合理化.
DOI:10.1039/c9Sc02126D

专利信息

专利号:US-2004106829-A1
优先权日:2002-11-12
标题 :Process for the synthesis of modafinil
发明人：FORNAROLI MIRCO; VELARDI FRANCESCO; COLLI CORRADO; BAIMA ROBERTO
权利人:PROCOS SPA
摘要:The present invention relates to a process for the preparation of 2-(benzhydrylthio)acetamide (II), key intermediate for the synthesis of modafinil, by reaction of benzhydryl chloride with thiourea and chloroacetamide.

专利号:US-9938509-B2
优先权日:2010-12-08
标 题 :Biocatalysts and methods for the synthesis of armodafinil
发明人：ANG EE LUI; ALVIZO OSCAR; BEHROUZIAN BEHNAZ; CLAY MICHAEL D; COLLIER STEVEN J; EBERHARD ELLEN D; FAN FU; SONG SHIWEI; SMITH DEREK J; WIDEGREN MAGNUS; WILSON ROBERT; XU JUNYE; ZHU JUN
权利人:CODEXIS INC
摘要:The present invention relates to non-naturally occurring polypeptides useful for preparing armodafinil, polynucleotides encoding the polypeptides, and methods of using the polypeptides. The non-naturally occurring polypeptides of the present invention are effective in carrying out biocatalytic conversion of the (i) 2-(benzhydrylsulfinyl)acetamide to (−)-2-[(R)-(diphenylmethyl)sulfinyl]acetamide (armodafinil), or (ii) benzhydryl-thioacetic acid to (R)-2-(benzhydrylsulfinyl)acetic acid, which is a pivotal intermediate in the synthesis of armodafinil, in enantiomeric excess.

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-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-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-2005222257-A1
优先权日:2003-09-19
标题:Process for enantioselective synthesis of single enantiomers of modafinil by asymmetric oxidation