Practical Synthesis of 6-Amino-1-hydroxy-2,1-benzoxaborolane: A Key Intermediate of DNDI-6148 [0.03%]
6-氨基-1-羟基-2,1-苯并氧杂硼烷的合成及其在DNDI-6148中的应用研究
Pankaj V Khairnar,John M Saathoff,Daniel W Cook et al.
Pankaj V Khairnar et al.
Visceral leishmaniasis (VL), a parasitic, poverty-linked, neglected disease, is endemic across multiple regions of the world and fatal if untreated. There is an urgent need for a better and more affordable treatment for VL. DNDI-6148 is a p...
Kilo-Scale GMP Synthesis of Renewable Semisynthetic Vaccine-Grade Squalene [0.03%]
千公斤规模的可再生半合成疫苗级鲨烯的GMP合成
Karl J Fisher,Laura Shirtcliff,Greg Buchanan et al.
Karl J Fisher et al.
Emulsions of the triterpene squalene ((6E,10E,14E,18E)-2,6,10,15,19,23-hexamethyltetracosa-2,6,10,14,18,22-hexaene, CAS 111-02-4) have been used as adjuvants in influenza vaccines since the 1990s. Traditionally sourced from shark liver oil,...
Development and Scale-Up of a New Sulfone-Based Bismacycle as a Universal Precursor for Bi(V)-Mediated Electrophilic Arylation [0.03%]
新型磺酮基双齿配体铋配合物的开发及其在Bi(V)介导的亲电芳基化反应中的应用研究
Andrew Fox,Liam T Ball
Andrew Fox
The scope and practical utility of bismuth(V)-mediated electrophilic arylation have been greatly improved by the recent development of user-friendly protocols based on modular bismacycle reagents. Here, we report the scalable synthesis of a...
Highly Regioselective Protecting-Group-Free Synthesis of the Antimalarial Drug MMV693183 [0.03%]
新型抗疟药物MMV693183的高度区域选择性无保护基合成法
Pankaj V Khairnar,Sarah L Aleshire,Ravi Kumar Ongolu et al.
Pankaj V Khairnar et al.
MMV693183 is a promising antimalarial drug candidate that works for uncomplicated malaria treatment and resistance management. Herein, we report an efficient and highly regioselective synthesis of MMV693183. This novel synthetic method high...
Correction to " N-Nitrosodimethylamine Formation in Metformin Drug Products by the Reaction of Dimethylamine and Atmospheric NO2" [0.03%]
《通过二甲胺和大气NO2的反应在盐酸二甲双胍制剂中形成N-亚硝基二甲胺》的更正
Shohei Fukuda,Kanako Kondo,Shoji Fukumoto et al.
Shohei Fukuda et al.
[This corrects the article DOI: 10.1021/acs.oprd.3c00274.]. © 2024 The Authors. Published by American Chemical Society.
Published Erratum
Organic process research & development. 2024 Jan 3;28(1):325. DOI:10.1021/acs.oprd.3c00473 2024
Process Development for the Manufacture of the Antimalarial Amodiaquine Dihydrochloride Dihydrate [0.03%]
抗疟疾药物Amodiaquine二盐酸盐二水合物的生产过程开发
Mukut Gohain,Modibo S Malefo,Phaladi Kunyane et al.
Mukut Gohain et al.
A robust process for the manufacture of the active pharmaceutical ingredient (API) amodiaquine dihydrochloride dihydrate (ADQ, 3), an important antimalarial, is reported. The process consists of a three-step synthetic route that involves a ...
Rapid Enantiomeric Excess Measurements of Enantioisotopomers by Molecular Rotational Resonance Spectroscopy [0.03%]
基于分子旋锁共振光谱学的enantioisotopomer的对映体过量快速测定法
Reilly E Sonstrom,Zoua Pa Vang,Haley N Scolati et al.
Reilly E Sonstrom et al.
Recent work in drug discovery has shown that selectively deuterated small molecules can improve the safety and efficacy for active pharmaceutical ingredients. The advantages derive from changes in metabolism resulting from the kinetic isoto...
Application of Chiral Transfer Reagents to Improve Stereoselectivity and Yields in the Synthesis of the Antituberculosis Drug Bedaquiline [0.03%]
手性转移试剂在抗结核药物贝达奎林合成中的应用以提高立体选择性和收率
Juliana M S Robey,Sanjay Maity,Sarah L Aleshire et al.
Juliana M S Robey et al.
Bedaquiline (BDQ) is an important drug for treating multidrug-resistant tuberculosis (MDR-TB), a worldwide disease that causes more than 1.6 million deaths yearly. The current synthetic strategy adopted by the manufacturers to assemble this...
Impact of Additives on Drug Particles during Liquid Antisolvent Crystallization and Subsequent Freeze-Drying [0.03%]
添加剂对液抗溶剂结晶过程中药物颗粒及后续冻干品的影响
Peuli Ghosh,Ake Rasmuson,Sarah P Hudson
Peuli Ghosh
The impact of single or combinations of additives on the generation of nanosuspensions of two poorly water-soluble active pharmaceutical ingredients (APIs), fenofibrate (FF) and dalcetrapib (DCP), and their isolation to the dry state via an...
Short and Efficient Synthesis of the Antituberculosis Agent Pretomanid from (R)-Glycidol [0.03%]
由甘油衍生物(R)-环氧甘油醇高效合成抗结核药物Bpa718/PBT5402(Pretomanid)的新方法
Tobias Lucas,Jule-Philipp Dietz,Flavio S P Cardoso et al.
Tobias Lucas et al.
An efficient gram-scale synthesis of the antituberculosis agent pretomanid using straightforward chemistry, mild reaction conditions, and readily available starting materials is reported. Four different protecting groups on the glycidol moi...