欧盟法规
ECHA物质C&L通报REACH预注册1-(3-二甲基氨基丙基)-3-乙基碳二亚胺,碘甲烷 以 二氯甲烷 用作溶剂,化学反应 1.0H,以81.2%的收率获得二甲基氨基丙基乙基碳酰胺
参考文献:一种1-乙基-3-(3-二甲胺基丙基)碳二亚胺碘甲烷的合成方法
标题:一种1-乙基-3-(3-二甲胺基丙基)碳二亚胺碘甲烷的合成方法
摘要:本发明的一种1‑乙基‑3‑(3‑二甲胺基丙基)碳二亚胺碘甲烷的合成方法,包括如下步骤:步骤一,一反应釜中加入二氯甲烷溶剂4.3公斤,投入1‑乙基‑3‑(3‑二甲基氨基丙基)‑碳化二亚胺搅拌均匀后,将混合液降至设定温度15oc以下,得到混合溶液a;步骤二,在混合溶液a中滴加碘甲烷,控制混合溶液a与碘甲烷的反应温度为15oc~25°C,滴加碘甲烷结束后继续反应1小时,其反应温度控制在25oc以下,得到混合溶液b;步骤三,混合溶液b加入石油醚溶剂,保温2小时,温度控制在25oc以下;步骤四,将步骤三反应生成的物料真空干燥,得到1‑乙基‑3‑(3‑二甲基氨基丙基)‑碳化二亚胺碘甲烷成品.
专利信息
专利号:US-2024239791-A1
优先权日:2021-04-26
标题 :Processes for the synthesis of valbenazine
发明人:TUCKER JOHN LLOYD
权利人:NEUROCRINE BIOSCIENCES INC
摘要:The present application relates to processes for preparing (S)-(2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b-hexahydro-1H-pyrido[2,1-a]isoquinolin-2-yl 2-amino-3-methylbutanoate di(4-methylbenzenesulfonate), which is an inhibitor of vesicular monoamine transporter 2 (VMAT2) useful in the treatment of hyperkinetic movement disorders such as tardive dyskinesia (TD).
专利号:US-2022363680-A1
优先权日:2019-09-13
标题 :Processes for the synthesis of valbenazine
发明人:TUCKER JOHN; KUCERA DAVID; HETTINGER DONALD; COCHRAN BRIAN M; BRANUM SHAWN; LE JACKIE; MCGEE KEVIN
权利人:NEUROCRINE BIOSCIENCES INC
摘要:The present application relates to processes for making (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b -hexahydro-1H-pyrido[2,1-a]isoquinolin-2-yl (S)-2-amino-3-methylbutanoate di(4-methylbenzenesulfonate), which is an inhibitor of vesicular monoamine transporter 2 (VMAT2) useful in the treatment of hyperkinetic movement disorders such as tardive dyskinesia (TD).
专利号:US-9035070-B2
优先权日:2010-07-30
标 题 :Process for the preparation of 1-aryl-pyrazol-3-one intermediates useful in the synthesis of sigma receptors inhibitors
发明人:BARTRA SANMARTI MARTÃ?; BERENGUER MAIMO RAMON; MEDRANO RUPEREZ JORGE; GARCIA GOMEZ JORGE; ARIZA PIQUER JAVIER
权利人:BARTRA SANMARTI MARTÃ?; BERENGUER MAIMO RAMON; MEDRANO RUPEREZ JORGE; GARCIA GOMEZ JORGE; ARIZA PIQUER JAVIER; ESTEVE QUÃ?MICA S A
摘要:The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.
专利号:US-6441189-B1
优先权日:2000-03-31
标 题 :Process for the preparation of matrix metalloproteinase inhibitors
发明人:BAILEY ANNE E; HILL DAVID R; HSIAO CHI-NUNG W; KURUKULASURIYA RAVI; WITTENBERGER STEVE; MCDERMOTT TODD; MCLAUGHLIN MAUREEN A
权利人:ABBOTT LAB
摘要:The instant invention provides a process for the synthesis of matrix metalloproteinase inhibitors.
专利号:US-9303014-B2
优先权日:2013-05-01
标题:Synthesis of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2,6-dione
发明人:RUCHELMAN ALEXANDER L; COHEN BENJAMIN M; CHOUDHURY ANUSUYA; KREILEIN MATTHEW M; LEONG WILLIAM W; MAN HON-WAH
权利人:CELGENE CORP
摘要:Provided herein are processes for the preparation of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2,6-dione, or an enantiomer or a mixture of enantiomers thereof; or a pharmaceutically acceptable salt thereof.
专利号:WO-2024146948-A1
优先权日:2023-01-05
标题:Peptide synthesis method involving sterically hindered tri-tert-butyl-tryptophan (tbt) residue
发明人:EKSTEEN JACOBUS JOHANNES; SVENDSEN JOHN SIGURD; MALMEDY FLORENCE; GUEVARA JONATHAN
权利人:AMICOAT AS
摘要:The invention is directed to a method of peptide synthesis comprising reacting a compound of Formula (I) or a salt thereof with a carbodiimide reagent to form an O-acylisourea intermediate; reacting the O-acylisourea intermediate with an additive to form an activated ester; and reacting the activated ester with an amino-containing moiety which is an amino acid, a peptide or a salt thereof comprising an amino group, wherein the amino group forms an amide bond with the carbonyl marked * in Formula (I); wherein the compound of Formula (I) has the structure: and wherein R1 and R2 are as defined in the disclosure. The invention is also directed to a compound of Formula (III) as defined in the disclosure or a salt thereof.