CAS: 1629229-37-3; (R)-(4-Fluorophenyl)(8-Methyl-3-(3-Methyl-1,2,4-Thiadiazol-5-yl)-5,6-Dihydro-[1,2,4]Triazolo[4,3-A]Pyrazin-7(8H)-yl)Methanone

(R)-1-(2,4-Dimethoxybenzyl)-5-Ethoxy-6-Methyl-1,2,3,6-Tetrahydropyrazine置于碳酸氢钠,三氟乙酸体系中,用 甲醇,二氯甲烷 用作溶剂,化学反应 9.42H,反应生成非唑奈坦
参考文献:Optimization Of Novel Antagonists To The Neurokinin-3 Receptor For The Treatment Of Sex-Hormone Disorders (Part Ii)
标题:Optimization Of Novel Antagonists To The Neurokinin-3 Receptor For The Treatment Of Sex-Hormone Disorders (Part Ii)
摘要:Further Lead Optimization On N-Acyl-Triazolopiperazine Antagonists To The Neurokinin-3 Receptor (Nk3R) Based On The Concurrent Improvement In Bioactivity And Ligand Lipophilic Efficiency (Lle) Is Reported. Overall,Compound 3 (Lle > 6) Emerged As The Most Efficacious In Castrated Rat And Monkey To Lower Plasma Lh,And It Displayed The Best Off-Target Safety Profile That Led To Its Clinical Candidate Nomination For The Treatment Of Sex-Hormone Disorders.
Doi:10.1021/acsmedchemlett.5B00117

专利信息

专利号:US-12162849-B2
优先权日:2018-12-21
标题 :Synthesis of 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or of the methyl-d3 deuterated form thereof
发明人：HOVEYDA HAMID; DUTHEUIL GUILLAUME
权利人:OGEDA SA
摘要:The present invention relates to a method of synthesis of compound (I), wherein R1 represents methyl or methyl-d3, thus corresponding to 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or to the methyl-d3 deuterated form thereof. These compounds are useful as key intermediates in the synthesis of pharmaceutical compounds, especially fezolinetant and deuterated fezolinetant.

专利号:US-10787458-B2
优先权日:2014-09-25
标 题:Chiral synthesis of N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-A]pyrazines
发明人：HOVEYDA HAMID; DUTHEUIL GUILLAUME
权利人:OGEDA SA
摘要:Disclosed is a novel chiral synthesis of N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines of Formula (I): n nor a solvate thereof. The novel chiral synthesis avoids the use of protection/deprotection steps.

专利号:WO-2025210277-A1
优先权日:2024-04-05
标 题 :Synthesis of intermediates for the preparation of neurokinin-3 receptor antagonists
发明人：BARRECA GIUSEPPE; RONZONI SILVANO; FALZONI MARIANNA; FERRANTE LUCA; FORNARA MATTHIEU; TADDEI MAURIZIO; VINCIARELLI GIORGIA
权利人:QUIM SINTETICA S A
摘要:The present invention relates to synthetic processes for the preparation of compounds having activity as neurokinin-3-receptor antagonists, among which Fezolinetant, and of intermediates useful in the synthesis thereof.

专利号:WO-2020128003-A1
优先权日:2018-12-21
标 题 :SYNTHESIS OF 3-METHYL-1,2,4-THIADIAZOLE-5-CARBOHYDRAZIDE OR OF THE METHYL-d3 DEUTERATED FORM THEREOF

专利号:ES-2950143-T3
优先权日:2018-12-21
标 题 :Synthesis of 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or the deuterated methyl-d3 form of this

专利号:MX-2021007505-A
优先权日:2018-12-21
标题:SYNTHESIS OF 3-METHYL-1,2,4-THIADIAZOLE-5-CARBOHYDRAZIDE OR ITS DEUTERATED FORM WITH METHYL-D3.