Continuous-Flow Preparation of γ-Butyrolactone Scaffolds, 2-(5,5-dimethyl-2-oxotetrahydrofuran-3- yl)acetic acid

It’s only fair to share… (5,5-dimethyl-2-oxotetrahydrofuran-3-yl)acetic acid 2-(5,5-Dimethyl-2-oxotetrahydrofuran-3-yl)acetic acid 2-carboxymethyl-4-methyl-4-pentanolide, Cas 412298-86-3       2-(5,5-Dimethyl-2-oxotetrahydrofuran-3-yl)acetic acid (4a). 1H NMR (DMSO-d6, 400 MHz): δ = 3.20 – 3.10 (m, 1H), 2.62 (dd, J = 17.1, 4.4 Hz, 1H), 2.54 – 2.45 (m, 1H), 2.31 – 2.21 (m, 1H), 1.84 (t, J = 12.0 Hz, 1H), 1.39 …

FDA approves first biosimilar Herceptin (trastuzumab) for the treatment of certain breast and stomach cancers

It’s only fair to share… FDA approves first biosimilar for the treatment of certain breast and stomach cancers Ogivri, a biosimilar to the cancer drug Herceptin, is approved for HER2+ breast cancer and metastatic stomach cancers The U.S. Food and Drug Administration today approved Ogivri (trastuzumab-dkst) as a biosimilar to Herceptin (trastuzumab) for the treatment …

Palladium-catalyzed direct C-H ethoxycarbonylation of 2-aryl-1,2,3-triazoles and efficient synthesis of suvorexant

It’s only fair to share…   Palladium-catalyzed direct C-H ethoxycarbonylation of 2-aryl-1,2,3-triazoles and efficient synthesis of suvorexant Org. Chem. Front., 2018, Advance Article DOI: 10.1039/C7QO00945C, Research Article Rui Sang, Yang Zheng, Hailong Zhang, Xiaohua Wu, Qiantao Wang, Li Hai, Yong Wu Palladium-catalyzed direct ethoxycarbonylation with diethyl azodicarboxylate was developed and its reaction mechanism was explored …

VOXELOTOR

It’s only fair to share… VOXELOTOR GBT 440; GTx-011, Treatment of Sickle Cell Disease RN: 1446321-46-5 UNII: 3ZO554A4Q8 Molecular Formula, C19-H19-N3-O3, Molecular Weight, 337.3771 Benzaldehyde, 2-hydroxy-6-((2-(1-(1-methylethyl)-1H-pyrazol-5-yl)-3-pyridinyl)methoxy)- 2-hydroxy-6-((2-(1-(propan-2-yl)-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde Originator Global Blood Therapeutics Class Antianaemics; Small molecules Mechanism of Action Abnormal haemoglobin modulators; Sickle haemoglobin modulators Orphan Drug Status Yes – Sickle cell anaemia New Molecular Entity Yes Highest Development Phases Phase III Sickle cell anaemia Phase …

The synthesis, biological evaluation and structure–activity relationship of 2-phenylaminomethylene-cyclohexane-1,3-diones as specific anti-tuberculosis agents

It’s only fair to share… CAS  74102-02-6 Molecular Formula: C15H17NO3 Molecular Weight: 259.305 g/mol 2-(((2-hydroxyphenyl)amino)methylene)-5,5-dimethylcyclohexane-1,3-dione (39): White solid; m.p. 249 o C; TLC Rf value, 0.48 (in EtOAc:Hexane,60:40); IR (neat) 2980, 2950, 1678, 1040 cm-1; 1 H NMR (400 MHz, CD3OD) δ 9.86 (1H, bs), 8.66 (1H, d, J = 16.0 Hz), 7.46- 7.34 (1H, m), …

2,4-dimorpholinocyclopent-2-enone

It’s only fair to share…   1465003-25-1 cas   2,4-dimorpholinocyclopent-2-enone (1b): 1H NMR (300 MHz, CDCl3) 6.24 (d, J = 2.9 Hz, 1H, COC=CH), 3.78 (t, J = 4.7 Hz, 4H, morpholine), 3.73 (t, J = 4.7 Hz, 4H, morpholine), 3.73-3.72 (m, 1H, COCH2CHN), 3.15-3.14 (m, 4H, morpholine), 2.54-2.52 (m, 4H, morpholine), 2.49-2.48 (m, 1H, …

Copanlisib

It’s only fair to share… Copanlisib, BAY 80-6946,  BAY 84-1236 Molecular FormulaC23H28N8O4 Average mass480.520 Da Cas 1032568-63-0 [RN] 1402152-26-4 MONO HCL UNII-WI6V529FZ9 FDA Approved September 2017 2-Amino-N-{7-methoxy-8-[3-(4-morpholinyl)propoxy]-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl}-5-pyrimidinecarboxamide 5-Pyrimidinecarboxamide, 2-amino-N-[2,3-dihydro-7-methoxy-8-[3-(4-morpholinyl)propoxy]imidazo[1,2-c]quinazolin-5-yl]- orphan drug status for follicular lymphoma Copanlisib (BAY 80-6946), developed by Bayer, is a selective Class I phosphoinositide 3-kinase inhibitor[1] which has shown promise in Phase I/II clinical trials for the treatment of non-Hodgkin lymphoma and chronic lymphocytic leukemia.[2] …

4-methyl-2-phenylbenzoxazole

It’s only fair to share…     4-methyl-2-phenylbenzoxazole 77791-11-8 4-methyl-2-phenylbenzoxazole (2b) [ref] White solid, 39mg, isolated yield 94%. 1H NMR (400 MHz, CDCl3) δ 8.17 (dd, J = 6.6, 3.0 Hz, 2H), 7.49 – 7.37 (m, 3H), 7.30 (d, J = 8.0 Hz, 1H), 7.14 (t, J = 7.7 Hz, 1H), 7.04 (d, J = …

TAFAMIDIS

It’s only fair to share… Tafamidis Molecular Formula C14H7Cl2NO3 Average mass 308.116 Da TAFAMIDIS, Fx-1006A PF-06291826 2-(3,5-Dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid 594839-88-0 [RN] 6-Benzoxazolecarboxylic acid, 2-(3,5-dichlorophenyl)- Vyndaqel Tafamidis meglumine Familial amyloid polyneuropathy LAUNCHED PFIZER 2011 EU ApprovedJapanese Pharmaceuticals and Medical Devices Agency in September 2013 PHASE 3, at  FDA, Amyloidosis, PFIZER Molecular Formula: C21H24Cl2N2O8 Molecular Weight: 503.329 g/mol CAS 951395-08-7 http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002294/WC500117838.pdf D-Glucitol, 1-deoxy-1-(methylamino)-, 2-(3,5-dichlorophenyl)-6-benzoxazolecarboxylate Tafamidis (INN, or Fx-1006A,[1] trade …

Pracinostat

It’s only fair to share… Pracinostat Molecular Formula C20H30N4O2 Average mass 358.478 Da 2-Propenamide, 3-[2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl]-N-hydroxy-, (2E)- 929016-96-6 [RN] SB939 (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1,3-benzodiazol-5-yl}-N-hydroxyprop-2-enamide N-hydroxy-1-[(4-methoxyphenyl)methyl]-1H-indole-6-carboxamide PCI 34051,  UNII: GPO2JN4UON 929016-98-8 DI HCl salt, C20 H30 N4 O2 . 2 Cl H, 431.4 929016-96-6 (free base) 929016-97-7 (trifluoroacetate) S*BIO (Originator) Leukemia, acute myeloid, phase 3, helsinn CAS 929016-98-8 DI HCl salt, C20 H30 N4 O2 . 2 Cl …