A Continuous Flow Sulfuryl Chloride-Based Reaction-Synthesis of a Key Intermediate in a New Route toward Emtricitabine and Lamivudine [0.03%]
一种新的合成恩曲他滨和拉米夫定关键中间体的连续流氯化硫酰基反应路线
Juliana M de Souza,Mateo Berton,David R Snead et al.
Juliana M de Souza et al.
We demonstrate a continuous two-step sequence in which sulfenyl chloride is formed, trapped by vinyl acetate, and chlorinated further via a Pummerer rearrangement. These reactions produce a key intermediate in our new approach to the oxathi...
Synthesis of an Oxathiolane Drug Substance Intermediate Guided by Constraint-Driven Innovation [0.03%]
受约束驱动创新指导的氧硫杂环药物原料中间体的合成
K Kashinath,David R Snead,Justina M Burns et al.
K Kashinath et al.
A new route was developed for construction of the oxathiolane intermediate used in the synthesis of lamivudine (3TC) and emtricitabine (FTC). We developed the presented route by constraining ourselves to low-cost, widely available starting ...
Development of an Effective Scalable Enantioselective Synthesis of the HIV-1 Entry Inhibitor BNM-III-170 as the Bis-Trifluoroacetate Salt [0.03%]
HIV-1 入胞抑制剂BNM-III-170的双三氟乙酸盐的有效可放大的不对称合成方法的开发
Junhua Chen,Jun Park,Sharon M Kirk et al.
Junhua Chen et al.
We report here the development and optimization of a process synthesis for the HIV-1 entry inhibitor BNM-III-170 bis-TFA salt (1). The synthesis features a dynamic-kinetic resolution (DKR) to establish the initial stereogenicity. By taking ...
Catalytic Enantioselective Synthesis of Chiral Organofluorine Compounds: Alcohol-Mediated Hydrogen Transfer for Catalytic Carbonyl Reductive Coupling [0.03%]
手性含氟化合物的催化不对称合成：醇介导的氢转移用于催化羰基还原偶联反应
Johannes Tauber,Leyah A Schwartz,Michael J Krische
Johannes Tauber
Alcohol-mediated carbonyl addition has enabled catalytic enantioselective syntheses of diverse fluorine-containing compounds without the need for stoichiometric metals or discrete redox manipulations. Reactions of this type may be separated...
Improved scale-up synthesis and purification of clinical asthma candidate MIDD0301 [0.03%]
临床哮喘候选药物MIDD0301改进的放大合成和纯化
Daniel E Knutson,Rashid Roni,Yeunus Mian et al.
Daniel E Knutson et al.
We report an improved and scalable synthesis of MIDD0301, a positive GABAA receptor modulator that is under development as oral and inhaled treatments for asthma. In contrast to other benzodiazepines in clinical use, MIDD0301 is a chiral co...
Scale-Up of the Manufacturing Process To Produce Docetaxel-Loaded mPEG- b-p(HPMA-Bz) Block Copolymer Micelles for Pharmaceutical Applications [0.03%]
用于制药的载多西他赛mPEG-b-p(HPMA-Bz)嵌段共聚物胶束的生产放大过程
Jaleesa Bresseleers,Mahsa Bagheri,Gert Storm et al.
Jaleesa Bresseleers et al.
An efficient, scalable, and good manufacturing practice (GMP) compatible process was developed for the production of docetaxel-loaded poly(ethylene glycol)-b-poly(N-2-benzoyloxypropyl methacrylamide) (mPEG-b-p(HPMA-Bz)) micelles. First, the...
A Structured Approach To Cope with Impurities during Industrial Crystallization Development [0.03%]
工业结晶过程中处理杂质的结构化方法
Stephanie J Urwin,Guillaume Levilain,Ivan Marziano et al.
Stephanie J Urwin et al.
The perfect separation with optimal productivity, yield, and purity is very difficult to achieve. Despite its high selectivity, in crystallization unwanted impurities routinely contaminate a crystallization product. Awareness of the mechani...
Scalable Synthesis of Esp and Rhodium(II) Carboxylates from Acetylacetone and RhCl3· x H2O [0.03%]
乙酰丙酮和氯化Rh(III)水合物制备esp和Rh(II)羧酸酯的可扩展合成法
Elisa Martínez-Castro,Samuel Suárez-Pantiga,Abraham Mendoza
Elisa Martínez-Castro
Rhodium(II) carboxylates are privileged catalysts for the most challenging carbene-, nitrene-, and oxo-transfer reactions. In this work, we address the strategic challenges of current organic and inorganic synthesis methods to access these ...
An Economical Route to Lamivudine Featuring a Novel Strategy for Stereospecific Assembly [0.03%]
一项经济高效合成拉米夫定的方法 featured 一种立体选择性构建的新策略
David R Snead,D Tyler McQuade,Saeed Ahmad et al.
David R Snead et al.
An economical synthesis of lamivudine was developed by employing a new method to establish the stereochemistry about the heterocyclic oxathiolane ring. Toward this end, an inexpensive and readily accessible lactic acid derivative served the...
Toward Sustained Product Formation in the Liquid-Phase Hydrogenation of Mandelonitrile over a Pd/C Catalyst [0.03%]
钯/碳催化剂下苦杏仁腈液相加氢长时间稳定生成苯乙酮的研究
Mairi I McAllister,Cédric Boulho,Colin Brennan et al.
Mairi I McAllister et al.
The liquid-phase hydrogenation of the aromatic cyanohydrin mandelonitrile (MN, C6H5CH(OH)CN) over a carbon-supported Pd catalyst to produce the primary amine phenethylamine (PEA, C6H5CH2CH2NH2) is investigated with respect to the transition...