📜D-色氨酸置于盐酸,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,三乙胺,3-羟基-1,2,3-苯并三嗪-4(3H)-酮体系中,用 二氯甲烷,乙酸乙酯 用作溶剂,化学反应 20.0H,反应生成阿拉莫林 参考文献:A Practical Synthesis Of The Pseudotripeptide Rc-1291 标题:A Practical Synthesis Of The Pseudotripeptide Rc-1291 摘要:The Rapid Process Development Of A Scaleable Synthesis Of The Pseudotripeptide Rc-1291 For Preclinical And Clinical Evaluation Is Described. By Employing A Nontraditional N-To-C Coupling Strategy,The Peptide Chain Of Rc-1291 Was Assembled In High Yield,With Minimal Racemization And In An Economical Manner By Introducing The Most Expensive Component Last. A One-Pot Deprotection/crystallization Procedure Was Developed For The Isolation Of Rc-1291 Free Base,Which Afforded The Target Compound In Excellent Yield And With A Purity Of > 99.5% Without Chromatographic Purification. Doi:10.1021/op0502506
专利号:IT-201800009235-A1 优先权日:2018-10-08 标题 :Process for the synthesis of exosomes containing heat shock proteins and their use for the treatment of muscle atrophy and cachexia
专利号:EP-2644618-B1 优先权日:2007-02-09 标题 :tether intermediates for the synthesis of macrocyclic ghrelin receptor modulators
专利号:EP-2644618-A1 优先权日:2007-02-09 标题:tether intermediates for the synthesis of macrocyclic ghrelin receptor modulators
专利号:WO-2024114661-A1 优先权日:2022-12-01 标题 :7-azaindole compounds, preparation method therefor, and use thereof 发明人:DONG XIAOCHUN; ZHANG XIONGWEN; ZHAO WEILI; Sun Weikuan; RUAN LI; WANG XIAOTING; FAN RONG; GU XIAOFAN 权利人:UNIV FUDAN; UNIV EAST CHINA NORMAL 摘要:Disclosed in the present invention are 7-azaindole compounds, a preparation method therefor, and the use thereof, belonging to the field of drug synthesis. The present invention particularly relates to 7-azaindole compounds containing pyrazole or indole substitution represented by general formula (I), a preparation method therefor, and the use thereof in medicine. The compounds of the present invention alleviate cancer cachexia skeletal muscle atrophy by means of inhibiting ActRIIB protein in the MSTN pathway, thereby achieving a remarkable anti-cancer-cachexia effect. Experimental results show that the compounds have good anti-cachexia activity and thus can further be used for preparing novel anti-cachexia drugs.
专利号:CN-117384063-A 优先权日:2023-08-29 标题:A kind of synthesis process and product of trimethylhydrazine
1: Matsukane R, Minami H, Fujimori N, Ueda K, Komori Y, Takamatsu Y, Ueda T, Kimura M, Matsuzaki C, Tanaka T, Morito A, Kuwahara S, Hashimoto M, Hirai S, Yokoyama T, Ishida S, Hirota T, Ogawa Y, Uchida M. Prospective study of anamorelin in pancreatic cancer cachexia: Clinical and translational insights into response heterogeneity. Clin Nutr. 2026 Jan 20;58:106581. doi: 10.1016/j.clnu.2026.106581. Epub ahead of print. 13(11):e70398. doi: 10.1002/rcr2.70398. 4: Yamamoto K, Kurokawa Y, Miyazaki Y, Omori T, Yanagimoto Y, Shinno N, Takeno A, Kawabata R, Akamaru Y, Sugimura K, Matsuyama J, Kimura Y, Yamashita K, Saito T, Takahashi T, Yamada T, Eguchi H, Doki Y. Efficacy and safety of anamorelin for cancer cachexia in patients with unresectable or recurrent gastric cancer: a multicentre, open-label, randomised controlled trial. EClinicalMedicine. 2025 Sep 22;88:103500. doi: 10.1016/j.eclinm.2025.103500. 5: Yoshida D, Ishimatsu M, Nakashima S, Nakano K, Ishida S, Orimoto H, Miyagahara T, Yada K, Matsumoto T, Kawanaka H. Impact of the Timing of Initial Anamorelin Administration in Advanced Gastrointestinal Cancer With Cancer Cachexia. In Vivo. 2025 Nov-Dec;39(6):3406-3411. doi: 10.21873/invivo.14137.
合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).