CAS: 161735-79-1; (R)-N-(Prop-2-Yn-1-yl)-2,3-Dihydro-1H-Inden-1-Amine Methanesulfonate

相似化合物

1875-50-9 1400989-19-6 202464-89-9

上下游产品

methanesulfonic acid rasagiline N-(2,3 dibromopropyl)-1-aminoindan 2,3-dihydro-1H-inden-1-aminerasagiline

1-茚酮肟置于candida Antarctica Lipase B,三乙醇胺,Palladium 10% On Activated Carbon,Pd/alo(Oh),氢气,Potassium Carbonate,Sodium Hydroxide体系中,用 乙醇,水,异丙醇,甲苯,乙腈 用作溶剂,化学反应 34.75H,反应生成甲磺酸雷沙吉兰
参考文献:化学动力学动态拆分合成雷沙吉兰的新方法
标题:化学动力学动态拆分合成雷沙吉兰的新方法
摘要:以南极假丝酵母脂肪酶b(calb)和pd纳米催化剂为催化剂,以动态动力学拆分(dkr)为关键步骤,提出了制备雷沙吉兰甲磺酸雷沙吉兰的新方法.通过外消旋氨基茚满rac-1的dkr获得手性中间体(R)-2,3-二氢-1-茚满胺,产率高(＞ 90%),对映选择性优异(ee＞ 99%).该过程可以在200克/升的73克规模下进行.甲磺酸雷沙吉兰在7个步骤中以25%的总收率和出色的对映选择性(99.9%ee)合成.
Doi:10.1021/op500152G

专利信息

专利号:US-8901352-B2
优先权日:2011-01-13
标题 :Method for the synthesis of rasagiline
发明人：REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN
权利人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN; NOBEL ILAÇ SANAYII VE TICARET A S
摘要:We have developed a new method for the synthesis of Rasagiline (Formula 1) based on the alkylation of trifluoroacetyl protected aminoindan. This protection enabled us to carry out an alkylation of aminoindan with a high yield and purity under very mild conditions with a wide range of reaction conditions and reagent selection. Considering the ease, purity and high yields of introducing and removal of the trifluoroacetyl group, this approach is a highly practical and economical way for the synthesis of rasagiline or its pharmaceutically acceptable salts.

专利号:US-12201669-B2
优先权日:2021-03-11
标 题:Small molecule suppressors of APOE gene expression and cerebral vascular amyloid pathology
发明人：TSAI LI-HUEI; BLANCHARD JOEL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present disclosure provides methods of inhibiting amyloid synthesis in a subject using small molecule inhibitors. The invention also includes methods of treating disease associated with amyloid synthesis, such as Alzheimer's disease. The small molecule inhibitors disclosed herein are compounds which are non-immunosuppressant cyclosporin including the pharmaceutically acceptable salts thereof.

专利号:WO-2009081148-A1
优先权日:2007-12-24
标 题:Process for the synthesis of propargylated aminoindan derivatives

专利号:CA-2708820-A1
优先权日:2007-12-24
标题 :Process for the synthesis of propargylated aminoindan derivatives

专利号:AU-2008339607-A1
优先权日:2007-12-24
标题:Process for the synthesis of propargylated aminoindan derivatives

专利号:EP-2663545-A1
优先权日:2011-01-13
标 题 :A new method for the synthesis of rasagiline