首页 > 化学

Pd-Catalyzed Arylation in the Synthesis of a GABA r2/3 Agonist

有机合成与工艺文献分享 2025-03-28 08:51
文章摘要
本文报道了一种替代合成GABA α2/3-agonist候选药物62的方法，以支持临床试验。与初始合成59类似，由于所需的硼酸昂贵且产生废物，Suzuki–Miyaura偶联必须被替换。作者开发了一种多克规模的C-H活化方法，通过将类似的杂环60与芳基氯61偶联。作者提出，通过使用Bu4NHSO4作为添加剂，可以稳定阴离子Pd0物种，从而实现催化剂周转。反应优化表明，通过使用1,4-二氧六环作为溶剂在90°C下可以避免Dimroth重排产生的2-芳基化产物和双芳基副产物。芳基氯61替代了硼酸偶联伙伴，降低了成本并提高了方法的原子经济性。经过重结晶，C-H芳基化产物62的收率为87%。
Pd-Catalyzed Arylation in the Synthesis of a GABA r2/3 Agonist
查看文献： The Expedient Synthesis of 4,2‘-Difluoro-5‘-(7-trifluoromethyl- imidazo[1,2-a]pyrimidin-3-yl)biphenyl-2-carbonitrile, a GABA α2/3 Agonist
查看期刊：Organic Process Research & Development
阅读全文
本站注明稿件来源为其他媒体的文/图等稿件均为转载稿，本站转载出于非商业性的教育和科研之目的，并不意味着赞同其观点或证实其内容的真实性。如转载稿涉及版权等问题，请作者速来电或来函联系。
推荐文献
Accounts of Chemical Research Accounts of Chemical Research
Last Honors and Life Experiences of Bereaved Families in the Context of COVID-19 in Kashmir: A Qualitative Inquiry About Exclusion, Family Trauma, and Other Issues.
DOI: 10.1177/00302228221134205 Pub Date : 2025-05-01 Date: 2022/10/26 0:00:00
IF 16.4 1区 化学 Q1
Accounts of Chemical Research
ACS Applied Polymer Materials ACS Applied Polymer Materials
Issue Editorial Masthead
DOI: 10.1021/apv007i007_192230810.1021/apv007i007_1922308 Pub Date : 2025-04-11
IF 4.4 2区 化学 Q2
ACS Applied Polymer Materials
Organic Process Research & Development Organic Process Research & Development
Access to Phenolic Pyridopyridazinones and Phthalazinones Using THP Ether-Directed Ortho Lithiation
DOI: 10.1021/acs.oprd.4c00541 Pub Date : 2025-04-15
IF 3.4 3区 化学 Q2
Organic Process Research & Development
最新文章
Evolution of the Process to an Advanced GPR40 Agonist (2)
Evolution of the Process to an Advanced GPR40 Agonist (2)
Org. Process Res. Dev. 2024, 28, 310−324. DOI: 10.1021/acs.oprd.3c00433◆Dibutylboron trifluoromethan
23小时前
Evolution of the Process to an Advanced GPR40 Agonist (1)
Evolution of the Process to an Advanced GPR40 Agonist (1)
Org. Process Res. Dev. 2024, 28, 310−324. DOI: 10.1021/acs.oprd.3c00433◆The medicinal chemistry rout
2025-04-14
Practical Synthesis of Chiral 3‑(Hydroxyiminomethyl)adipic Acid
Practical Synthesis of Chiral 3‑(Hydroxyiminomethyl)adipic Acid
Org. Process Res. Dev. 2023, 27, 2355−2364. DOI: 10.1021/acs.oprd.3c00320◆We examined three methodol
2025-04-14
First GMP Synthesis of SGD-9501-TFA (4)
First GMP Synthesis of SGD-9501-TFA (4)
Org. Process Res. Dev. 2024, 28, 3780−3790. DOI: 10.1021/acs.oprd.4c00318◆With access to activated l
2025-04-11
有机合成与工艺文献分享
Evolution of the Process to an Advanced GPR40 Agonist (2)
Evolution of the Process to an Advanced GPR40 Agonist (2) 23小时前
Evolution of the Process to an Advanced GPR40 Agonist (1)
Evolution of the Process to an Advanced GPR40 Agonist (1) 2025-04-14
Practical Synthesis of Chiral 3‑(Hydroxyiminomethyl)adipic Acid
Practical Synthesis of Chiral 3‑(Hydroxyiminomethyl)adipic Acid 2025-04-14
First GMP Synthesis of SGD-9501-TFA (4)
First GMP Synthesis of SGD-9501-TFA (4) 2025-04-11
First GMP Synthesis of SGD-9501-TFA (3)
First GMP Synthesis of SGD-9501-TFA (3) 2025-04-11
热门类别
综合性期刊 物理 法学 地球科学 历史学
相关文章
The Better Meat Co.获美专利：以马铃薯废料制真菌蛋白，加速全球布局 中古史图书馆 | 新书速递（2025年3月） 同济大学，Nature Synthesis！ The Innovation Geoscience | 末次冰盛期以来全球内流区湖泊碳埋藏及其未来预测 浙江大学，Nature Synthesis！
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号：481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们：info@booksci.cn
Book学术提供免费学术资源搜索服务，方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1