Practical and Scalable Synthetic Method for Preparation of Dolutegravir Sodium: Improvement of a Synthetic Route for Large-Scale Synthesis

It’s only fair to share… A practical and scalable synthetic method to obtain dolutegravir sodium (1) was established starting from the readily accessible material maltol (2). This synthetic method includes a scalable oxidation process of maltol and palladium-catalyzed amidation for introduction of an amide moiety, leading to a practical manufacturing method in short synthetic steps. …

Cenobamate

It’s only fair to share… Cenobamate CAS: 913088-80-9 Chemical Formula: C10H10ClN5O2 Molecular Weight: 267.67 Related CAS #: 913088-80-9   913087-59-9 Synonym: YKP-3089; YKP3089; YKP3089; Cenobamate IUPAC/Chemical Name: (R)-1-(2-chlorophenyl)-2-(2H-tetrazol-2-yl)ethyl carbamate 2H-Tetrazole-2-ethanol, α-(2-chlorophenyl)-, carbamate (ester), (αR)- (9CI) (1R)-1-(2-chlorophenyl)-2-(2H-tetrazol-2-yl)ethyl carbamate Carbamic acid (R)-(+)-1-(2-chlorophenyl)-2-(2H-tetrazol-2-yl)ethyl ester 2H-Tetrazole-2-ethanol, α-(2-chlorophenyl)-, 2-carbamate, (αR)- Cenobamate, also known as YKP-3089, is a novel new antiepileptic drug candidate. Cenobamate showed …

FOSTEMSAVIR ,фостемсавир , فوستيمسافير  , 磷坦姆沙韦  ,ホステムサビル;

It’s only fair to share… FOSTEMSAVIR ,фостемсавир , فوستيمسافير  , 磷坦姆沙韦  ,ホステムサビル; Fostemsavir GSK3684934 CAS 864953-29-7 Molecular FormulaC25H26N7O8P Average mass583.490 Da ホステムサビル; [3-[2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl]-4-methoxy-7-(3-methyl-1,2,4-triazol-1-yl)pyrrolo[2,3-c]pyridin-1-yl]methyl dihydrogen phosphate {3-[(4-Benzoyl-1-piperazinyl)(oxo)acetyl]-4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-1-yl}methyl dihydrogen phosphate [ACD/IUPAC Name] 1,2-Ethanedione, 1-(4-benzoyl-1-piperazinyl)-2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]- [ACD/Index Name] 10292 864953-29-7 [RN] фостемсавир [Russian] [INN] فوستيمسافير [Arabic] [INN] 磷坦姆沙韦 [Chinese] [INN] BMS 663068 BMS663068 Fostemsavir tromethamine UNII-2X513P36U0   Fostemsavir tromethamine [USAN], CAS 864953-39-9, MW 704.6303 Prodrug of BMS-626529, an HIV-1 attachment inhibitor. …

Rovafovir Etalafenamide

It’s only fair to share… Rovafovir etalafenamide GS-9131 UNII-U8S0IC8DY7  ethyl ((S)-((((2R,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-2,5-dihydrofuran-2-yl)oxy)methyl)(phenoxy)phosphoryl)-L-alaninate L-Alanine, N-((S)-((((2R,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-2,5-dihydro-2-furanyl)oxy)methyl)phenoxyphosphinyl)-, ethyl ester CAS: 912809-27-9 Chemical Formula: C21H24FN6O6P Molecular Weight: 506.43 Originator Gilead Sciences Class Antiretrovirals; Purine nucleosides; Small molecules Mechanism of Action Nucleoside reverse transcriptase inhibitors Phase II HIV-1 infections 03 Apr 2018 Phase-II clinical trials in HIV-1 infections (Treatment-experienced) in Uganda (PO) (NCT03472326) 21 Mar 2018 Gilead …

OLACAFTOR, VX 440

It’s only fair to share… OLACAFTOR, VX 440 CAS 1897384-89-2 Molecular Formula: C29H34FN3O4S Molecular Weight: 539.666 g/mol CFTR corrector; UNII-RZ7027HK8F; RZ7027HK8F; Target-based Actions, CFTR modulator Indications, Cystic fibrosis CS-0044588 UNII-RZ7027HK8F RZ7027HK8F Olacaftor (VX-440, VX440) is a next-generation CFTR corrector, shows the potential to enhance the amount of CFTR protein at the cell’s surface and for treatment of …

Development of an Efficient Manufacturing Process for a Key Intermediate in the Synthesis of Edoxaban

It’s only fair to share… Development of an Efficient Manufacturing Process for a Key Intermediate in the Synthesis of Edoxaban Makoto Michida*† , Hideaki Ishikawa†, Takeshi Kaneda†, Shinya Tatekabe‡, and Yoshitaka Nakamura§ †Process Technology Research Laboratories (PTRL), Daiichi Sankyo Co., Ltd., 1-12-1 Shinomiya, Hiratsuka-shi, Kanagawa 254-0014, Japan ‡Plant Management Department, Daiichi Sankyo Chemical Pharma Co., Ltd., 477 Takada, Odawara-shi, Kanagawa 250-0216, Japan §Global Supply Chain – Technology Function, Daiichi Sankyo, Inc., 211 Mt. Airy …

Viloxazine, ヴィロキサジン;

It’s only fair to share… Viloxazine Molecular FormulaC13H19NO3 Average mass237.295 Da 2-[(2-Ethoxyphenoxy)methyl]morpholine 256-281-7 [EINECS] 3489 46817-91-8 free [RN], Hcl 35604-67-2 5I5Y2789ZF Emovit [Wiki] Morpholine, 2-((2-ethoxyphenoxy)methyl)- Morpholine, 2-[(2-ethoxyphenoxy)methyl]- UNII:5I5Y2789ZF Viloxazine hydrochloride OQW30I1332 35604-67-2 Polymorph FORM A , B US226136693, US2011032013   Viloxazine (trade names Vivalan, Emovit, Vivarint and Vicilan) is a morpholine derivative and is a selective norepinephrine reuptake inhibitor (NRI). It was used as an antidepressant in some European countries, and produced …

Macimorelin acetate

It’s only fair to share… Macimorelin Molecular FormulaC26H30N6O3 Average mass474.555 Da CAS  381231-18-1 Chemical Formula: C26H30N6O3 Exact Mass: 474.23794 Molecular Weight: 474.55480 Elemental Analysis: C, 65.80; H, 6.37; N, 17.71; O, 10.11 2-Methylalanyl-N-[(1R)-1-formamido-2-(1H-indol-3-yl)ethyl]-D-tryptophanamide 381231-18-1 [RN] 8680B21W73 9073 D-Tryptophanamide, 2-methylalanyl-N-[(1R)-1-(formylamino)-2-(1H-indol-3-yl)ethyl]- CAS 945212-59-9 (Macimorelin acetate) (2R)-2-(2-amino-2-methylpropanamido)-3-(1H-indol-3-yl)-N-[(1R)-2-(1H-indol-3-yl)-1-formamidoethyl]propanamide; acetic acid AEZS-130 ARD-07 D-87875 EP-01572 EP-1572 JMV-1843 USAN (ab-26) MACIMORELIN ACETATE AQZ1003RMG …

Caplacizumab-yhdp, カプラシズマブ

It’s only fair to share… FDA approves first therapy Cablivi (caplacizumab-yhdp) カプラシズマブ  , for the treatment of adult patients with a rare blood clotting disorder FDA February 6, 2019 Release https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm630851.htm?utm_campaign=020919_PR_FDA%20approves%20therapy%20for%20treatment%20of%20adult%20patients%20with%20rare%20blood%20clotting%20disorder&utm_medium=email&utm_source=Eloqua The U.S. Food and Drug Administration today approved Cablivi (caplacizumab-yhdp) injection, the first therapy specifically indicated, in combination with plasma exchange and immunosuppressive therapy, …

Cannabidiol, カンナビジオール;

It’s only fair to share…   Cannabidiol カンナビジオール; Formula C21H30O2 CAS 13956-29-1 Mol weight 314.4617 FDA APPROVED, 2018/6/25, Epidiolex (Greenwich Biosciences) Efficacy Anticonvulsant, Antiepileptic, Cannabinoid receptor agonist Comment Treatment of seizures   1,3-Benzenediol, 2-[(1R,6R)-3-methyl-6-(1-methylethenyl)-3-cyclohexen-1-yl]-5-pentyl- 2-[(1R,6R)-6-Isopropenyl-3-methyl-3-cyclohexen-1-yl]-5-pentyl-1,3-benzenediol GWP42003-P UNII:19GBJ60SN5 GW Research Ltd  APH-1501 BRCX-014 BTX-1204 BTX-1503 CBD GW-42003 GWP-42003 GWP-42003-P PLT-101 PTL-101 ZYN-002 Cannabidiol CAS Registry Number: 13956-29-1 CAS Name: 2-[(1R,6R)-3-Methyl-6-(1-methylethenyl)-2-cyclohexen-1-yl]-5-pentyl-1,3-benzenediol …