CAS: 136236-51-6; (R)-N-(2-Propynyl)-2,3-Dihydroinden-1-Amine

该化合物是一种主要用于治疗帕金森病的选择性,不可逆的单胺氧化酶B(MAO-B)抑制剂,其特点是能够提高脑部多巴胺水平,从而减轻多巴胺的症状; 麻黄碱通常通过口服施用,以其...

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CAS号1224439-21-7 (R)-tert-butyl ... | CAS号161735-79-1 甲磺酸雷沙吉兰 | CAS号6165-76-0 对甲苯磺酸丙炔酯 | CAS号10277-74-4 (R)-(-)-1-氨基茚满 | CAS号6165-75-9 苯磺酸炔丙酯 | CAS号164294-89-7 acetic acid,(1R... | CAS号161735-79-1 甲磺酸雷沙吉兰

合成工艺路线路线简述

  • 合成目标产物 Rasagiline 主要起始原料 (R)-(-)-1-Aminoindan And 3-Chloropropyne
  • (文献来源)合成步骤主要原料 (R)-(-)-1-Aminoindan 和 3-Chloropropyne
甲磺酸雷沙吉兰 以 水 用作溶剂,化学反应 0.6H,反应生成雷沙吉兰
参考文献:Dosage Forms With An Enterically Coated Core Tablet
标题:Dosage Forms With An Enterically Coated Core Tablet
摘要:本发明提供了一种口服制剂给患者使用,包括一种经肠包被的核心片剂,套在压缩粉末或颗粒材料的环状体内.本发明还提供了一种联合使用两种或多种活性药物成分的药物剂型.本发明还提供了一种方法,包括将本发明的药物剂型用于患有胃动力障碍的患者,例如帕金森病患者.

海关参考信息

专利信息


专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

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-2006194971-A1
优先权日:2005-02-24
标 题 :Anethole dithiolethione and other dithiolethiones for the treatment of conditions associated with dysfunction of monoamine neruotransmission
发明人:DRUKARCH BENJAMIN; SCHOFFELMEER ANTON N; FEENSTRA ROELOF W; CHRISTEN MARIE-ODILE; BURGOT JEAN-LOUIS; CHOLLET MARYLENE; IWEMA BAKKER WOUTER I; VAN VLIET BERNARD J; TULP MARTINUS T
权利人:DRUKARCH BENJAMIN; SCHOFFELMEER ANTON N; FEENSTRA ROELOF W; CHRISTEN MARIE-ODILE; BURGOT JEAN-LOUIS; CHOLLET MARYLENE; IWEMA BAKKER WOUTER I; VAN VLIET BERNARD J; TULP MARTINUS T
摘要:The present disclosure relates to dithiolethione derivatives as monoamino oxidase inhibitors, in particular MAO-B inhibitors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said dithiolethiones derivatives. The present disclosure also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. In embodiments of the present disclosure specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment, amelioration or prevention of conditions associated with dysfunction of monoamine neurotransmission. The compounds have the general formula (1) n nwherein the symbols have the meanings given in the specification.

专利号:US-2008125354-A1
优先权日:2005-11-21
标题 :Selective inhibition of matrix metalloproteinases
发明人:FIELDS GREGG B; HAMMER ROBERT
权利人:UNIV FLORIDA ATLANTIC; UNIV LOUISIANA STATE
摘要:Synthetic triple-helical peptides (THPs) are used for the design and synthesis of triple-helical transition state analog inhibitors. These inhibitors feature a phosphonate ester or phosphinic moiety in place of the scissle bond. These groups inhibit MMPs, and methods been developed for their convenient incorporation within a peptide sequence by solid-phase methods.

专利号:US-8461388-B2
优先权日:2007-12-24
标题 :Process for the synthesis of propargylated aminoindan derivatives
发明人:PHULL MANJINDER SINGH; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO
权利人:PHULL MANJINDER SINGH; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; CIPLA LTD
摘要:A process for preparing a compound of formula (V) or its enantiomer, which comprises:n (a) reacting racemic aminoindan of formula (II) or its enantiomer with allylhalide in presence of a base and an organic solvent at a temperature ranging from 25 C to the reflux temperature of the solvent to give compound of formula (III); nn n n n n n n n n n n n Where R is n H or n n n n n n n n n n n n n n n n (b) reacting the compound (III) with halogenating agent in a suitable organic solvent to give a dihalo compound of formula (IV). n n n n n n n n n n n n n n n n (c) treating the dihalo compound (IV) with a suitable base to give compound (V).

专利号:US-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
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主要参考文献


1: Singh A, Sinha S, Singh NK. Dietary Natural Flavonoids: Intervention for MAO-B Against Parkinson's Disease. Chem Biol Drug Des. 2024 Sep;104(3):e14619. doi: 10.1111/cbdd.14619. 13(8):917. doi: 10.3390/antiox13080917.
3: Bovenzi R, Conti M, Pierantozzi M, Testone G, Fernandes M, Manfredi N, Schirinzi T, Cerroni R, Mercuri NB, Stefani A, Liguori C. Safinamide effect on sleep architecture of motor fluctuating Parkinson's disease patients: A polysomnographic rasagiline-controlled study. Parkinsonism Relat Disord. 2024 Aug 13;127:107103. doi: 10.1016/j.parkreldis.2024.107103. Epub ahead of print. 39(8):e4853. doi: 10.1002/bio.4853. 12(7):1592. doi: 10.3390/biomedicines12071592.
6: Matthews DC, Kinney JW, Ritter A, Andrews RD, Toledano Strom EN, Lukic AS, Koenig LN, Revta C, Fillit HM, Zhong K, Tousi B, Leverenz JB, Feldman HH, Cummings J. Relationships between plasma biomarkers, tau PET, FDG PET, and volumetric MRI in mild to moderate Alzheimer's disease patients. Alzheimers Dement (N Y). 2024 Jul 9;10(3):e12490. doi: 10.1002/trc2.12490.

合成参考文献


参考文献:10.1007/s10545-011-9375-8
摘要:Breuer ME, Willems PHGM, Russel FGM, Koopman WJH, Smeitink JAM. Modeling mitochondrial dysfunctions in the brain: from mice to men. J of Inher Metab Disea. 2011 Jul 14;35(2):193–210. doi: 10.1007/s10545-011-9375-8.
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