A5050830009- HIV/AIDS drug development and treatment
- Chemical Synthesis and Analysis
- Synthesis and Catalytic Reactions
- Analytical Chemistry and Chromatography
- Biochemical and Molecular Research
- Traditional and Medicinal Uses of Annonaceae
- Synthesis and Biological Evaluation
- Research on Leishmaniasis Studies
- Click Chemistry and Applications
- Chemical Synthesis and Reactions
- Cytomegalovirus and herpesvirus research
- Synthesis and Characterization of Heterocyclic Compounds
- Pharmacological Effects and Toxicity Studies
- HIV Research and Treatment
- Carbohydrate Chemistry and Synthesis
- Chemical Reactions and Isotopes
- Malaria Research and Control
- Asymmetric Synthesis and Catalysis
- Pneumocystis jirovecii pneumonia detection and treatment
- Radical Photochemical Reactions
- Phenothiazines and Benzothiazines Synthesis and Activities
- Alkaloids: synthesis and pharmacology
Virginia Commonwealth University
2023-2025
Association for Language Learning
2024
Herein, we describe a new five-step approach to prepare 1-(3,6-dibromopyridin-2-yl)-2-(3,5-difluorophenyl)ethan-1-amine, an important intermediate in the synthesis of lenacapavir. The key step sequence is Weinreb amide-based ketone synthesis, which provides alternative entry point core structural component. Starting from inexpensive 2-(3,5-difluorophenyl)acetic acid, amide and followed nucleophilic substitution afford 47% yield. subsequent functional group manipulation delivers racemic amine...
7-Bromo-4-chloro-1H-indazol-3-amine is a heterocyclic fragment used in the synthesis of Lenacapavir, potent capsid inhibitor for treatment HIV-1 infections. In this manuscript, we describe new approach to synthesizing 7-bromo-4-chloro-1H-indazol-3-amine from inexpensive 2,6-dichlorobenzonitrile. This synthetic method utilizes two-step sequence including regioselective bromination and heterocycle formation with hydrazine give desired product an overall isolated yield 38–45%. The protocol has...
(1R,5R)-2,2-Dimethoxybicyclo[3.1.0]hexan-3-one is used in the asymmetric synthesis of lenacapavir. Herein, we report an enantioselective this important chiral intermediate from inexpensive commodity (R)-epichlorohydrin. This synthetic method comprises 6 steps, including a 4-step telescoped bicyclic ketone synthesis, I2-promoted hydroxylation, and Albright–Goldman oxidation. sequence affords (1R,5R)-2,2-dimethoxybicyclo[3.1.0]hexan-3-one overall 25% isolated yield as enantiomerically pure...
Herein, we describe two practical approaches to synthesize (
Herein, we describe a new seven-step approach to prepare (S)-1-(3,6-dibromopyridin-2-yl)-2-(3,5-difluorophenyl)ethan-1-amine ((S)-4) from the inexpensive 2-(3,5-difluorophenyl)acetic acid. The key steps in sequence include (1) Weinreb amide-based ketone synthesis provide an entry point core structure; (2) simple functional group transformations afford racemic amine 4-rac; and (3) dynamic kinetic resolution (DKR) access chiral (S)-4. This process delivered enantiopure (S)-4 overall isolated...
Herein, we describe two practical approaches to synthesize (R)-(+)-1,2-epoxy-5-hexene from inexpensive and readily available raw materials reagents. The first approach is a two-step sequence, involving an epoxidation with meta-chloroperoxybenzoic acid (mCPBA) chiral resolution (salen)Co(II), producing in 24-30% of overall yield. second utilizes the (R)-epichlorohydrin as starting material features epoxide ring opening reaction allylMgCl NaOH mediated closure reaction. Development this...
7-Bromo-4-chloro-1H-indazol-3-amine is a heterocyclic fragment used in the synthesis of Lenacapavir, potent capsid inhibitor for treatment HIV-1 infections. In this manuscript, we describe new approach to synthesizing 7-bromo-4-chloro-1H-indazol-3-amine from inexpensive 2,6-dichlorobenzonitrile. This synthetic method utilizes two-step sequence including regioselective bromination and heterocycle formation with hydrazine give desired product an overall isolated yield 38-45%. The protocol has...
(1R,5R)-2,2-Dimethoxybicyclo[3.1.0]hexan-3-one is used in the asymmetric synthesis of lenacapavir. Herein, we report an enantioselective this important chiral intermediate from inexpensive commodity (R)-epichlorohydrin. This synthetic method comprises 6 steps, including a 4-step telescoped bicyclic ketone synthesis, I2-promoted hydroxylation, and Albright-Goldman oxidation. sequence affords (1R,5R)-2,2-dimethoxybicyclo[3.1.0]hexan-3-one overall 25% isolated yield as enantiomerically pure...
MMV693183 is a promising antimalarial drug candidate that works for uncomplicated malaria treatment and resistance management. Herein, we report an efficient highly regioselective synthesis of MMV693183. This approach to only three steps from readily available starting materials provides the API in 46 % overall yield without requiring protecting groups.
MMV693183 is a promising antimalarial drug candidate that works for uncomplicated malaria treatment and resistance management. Herein, we report an efficient highly regioselective synthesis of MMV693183. This novel synthetic method highlights three-step route with overall yield 46% from readily available starting materials. The key to the success lies in (1) utilizing subtle difference two amino groups material (S)-propane-1,2-diamine dihydrochloride without protection (2) identifying...
Visceral leishmaniasis (VL), a parasitic, poverty-linked, neglected disease, is endemic across multiple regions of the world and fatal if untreated. There an urgent need for better more affordable treatment VL. DNDI-6148 promising drug candidate being evaluated VL; however, current process producing key intermediate DNDI-6148, 6-amino-1-hydroxy-2,1-benzoxaborolane, expensive difficult to scale up. Herein, we describe two practical approaches synthesizing 6-amino-1-hydroxy-2,1-benzoxaborolane...