13861-75-1

Upstream product

• 422280-53-3 1-(2-nitro-phenyl)-cyclopropanecarboxylic acid 
• 88426-99-7 3-(2-Chloro-ethyl)-1,3-dihydro-indol-2-one 
• 79697-17-9 3-acetylspiroindol>-2'(1'H)-one 
• 88426-95-3 3-[2-(tosyloxy)ethyl]-2-indolinone 
• 3690-95-7 (+/-)-3-(2-hydroxy-ethyl)-1,3-dihydro-indol-2-one 
• 98-59-9 p-toluenesulfonyl chloride 
• 118-92-3 anthranilic acid 
• 64053-80-1 1'-acetylspiroindol>-3'(1'H)-one 
• 59-48-3 2-oxoindole 
• 247129-85-7 (2-bromoethyl)(diphenyl)sulfonium trifluoromethanesulfonate 
• 25250-89-9 2H-indol-2-one 
• 106-93-4 ethylene dibromide 
• 214610-10-3 N-boc-2-oxyindole 
• 1774-47-6 trimethylsulfoxonium iodide 

Downstream Products

• 875071-97-9 5'-bromospiro[cyclopropane-1,3'-indoline]-2'-one 
• 165379-18-0 N-(1-azabicyclo[2.2.2]octan-4-ylmethyl)-2'-oxo-spiro[cyclopropane-1,3'-[3'H]indole]-1'(2'H)-carboxamide 
• 618446-19-8 6-nitro-1,2-dihydro-3-spiro-1'-cyclopropyl-1H-indole 
• 1399663-06-9 C₁₀H₁₀N₂O 
• 1399654-82-0 5′-nitrospiro[cyclopropane-1,3′-indoline]-2′-one 
• 174-66-3 1',2'-dihydrospiroindole> 
• 1352949-88-2 3-((4-oxo-8-(3-(2'-oxospiro[cyclopropane-1,3'-indoline]-1'-yl)propyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoic acid hydrochloride 
• 1352950-46-9 tert-butyl 2-((1-(4-fluorophenyl)-4-oxo-8-(3-(2'-oxospiro[cyclopropane-1,3'-indoline]-1'-yl)propyl)-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoate 
• 1352950-18-5 tert-butyl 2-((4-oxo-8-(3-(2'-oxospiro[cyclopropane-1,3'-indoline]-1'-yl)propyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoate 
• 1352950-01-6 tert-butyl 3-((1-(4-fluorophenyl)-4-oxo-8-(3-(2'-oxospiro[cyclopropane-1,3'-indoline]-1'-yl)propyl)-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoate 

Relevant academic research and scientific papers

Discovery of Sisunatovir (RV521), an Inhibitor of Respiratory Syncytial Virus Fusion

RV521 is an orally bioavailable inhibitor of respiratory syncytial virus (RSV) fusion that was identified after a lead optimization process based upon hits that originated from a physical property directed hit profiling exercise at Reviral. This exercise encompassed collaborations with a number of contract organizations with collaborative medicinal chemistry and virology during the optimization phase in addition to those utilized as the compound proceeded through preclinical and clinical evaluation. RV521 exhibited a mean IC50 of 1.2 nM against a panel of RSV A and B laboratory strains and clinical isolates with antiviral efficacy in the Balb/C mouse model of RSV infection. Oral bioavailability in preclinical species ranged from 42 to >100% with evidence of highly efficient penetration into lung tissue. In healthy adult human volunteers experimentally infected with RSV, a potent antiviral effect was observed with a significant reduction in viral load and symptoms compared to placebo.

NOVEL COMPOUNDS USEFUL AS POLY(ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS

The present invention provides novel poly(ADP-ribose) polymerase (PARP) inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods for the treatment, prevention and/or amelioration of PARP mediated diseases or disorders using them. In particular, the compounds described herein are useful for the treatment of carcinoma of the breast, ovarian cancer, carcinoma of the liver, carcinoma of the lung, small cell lung cancer, esophageal cancer, gall bladder cancer, pancreatic cancer and stomach cancer.

Vinyl Thianthrenium Tetrafluoroborate: A Practical and Versatile Vinylating Reagent Made from Ethylene

The use of vinyl electrophiles in synthesis has been hampered by the lack of access to a suitable reagent that is practical and of appropriate reactivity. In this work we introduce a vinyl thianthrenium salt as an effective vinylating reagent. The bench-stable, crystalline reagent can be readily prepared from ethylene gas at atmospheric pressure in one step and is broadly useful in the annulation chemistry of (hetero)cycles, N-vinylation of heterocyclic compounds, and palladium-catalyzed cross-coupling reactions. The structural features of the thianthrene core enable a distinct synthesis and reactivity profile, unprecedented for other vinyl sulfonium derivatives.

Influenza virus replication inhibitors and uses thereof

The invention belongs to the field of medicines, and particularly relates to novel compounds serving as an influenza virus replication inhibitor, a preparation method thereof, a pharmaceutical composition containing the compounds and application of the compounds and the pharmaceutical composition in treatment of influenza. The compounds are compounds as shown in a formula (I) or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrugs of the stereoisomer, the tautomer, the nitrogen oxide, the solvate, the metabolite and the pharmaceutically acceptable salt of the compound as shown in the formula (I). The compounds not only can well inhibit influenza viruses, but also have lower cytotoxicity, excellent in-vivo pharmacokinetic property and the in-vivo pharmacodynamic property and good liver microsome stability.

LACTAM COMPOUND AS FXR RECEPTOR AGONIST

Disclosed is a compound as shown in formula (I), an optical isomer thereof or a pharmaceutically acceptable salt thereof, and the present invention relates to the use of same in the preparation of a drug for treating FXR-related diseases.

THIENODIAZEPINE DERIVATIVES AND APPLICATION THEREOF

The present invention relates to a class of thienodiazepine derivatives and an application thereof in the preparation of a drug for the treatment of diseases associated with bromodomain and extra-terminal (BET) Bromodomain inhibitors. Specifically, the present invention relates to compounds represented by formulas (I) and (II), as well as pharmaceutically acceptable salts thereof.

Rhodium(III)-Catalyzed Cyclopropane C-H/C-C Activation Sequence Provides Diastereoselective Access to α-Alkoxylated γ-Lactams

A Cp*Rh(III)-catalyzed C-H/C-C bond activation sequence of cyclopropyl hydroxamates has been developed. The three-component process allows trapping of the intermediate rhodacycle with diazomalonates and an alcohol nucleophile to provide access to synthetically valuable α-alkoxylated γ-lactams with trans diastereoselectivity.

A convenient cyclopropanation process of oxindoles via bromoethylsulfonium salt

A practical convenient conversion of oxindoles into the corresponding spirocyclopropyl oxindoles is achieved efficiently using bromoethylsulfonium salt, which is easily prepared on a large scale and is stable crystalline. This reaction of bromoethylsulfonium salt with different substituted unprotected oxindoles proceeded under mild condition and provided moderate yields.

Domino Corey-Chaykovsky Reaction for One-Pot Access to Spirocyclopropyl Oxindoles

The development of the sequential Corey-Chaykovsky reactions of isatins, spiroepoxy-, or spiroaziridine oxindoles with sulfur ylide has led to the discovery of a unique reaction mode that allows easy and direct one-pot access to a range of spirocyclopropyl oxindoles.

Synthesis of Oxindoles and Benzofuranones via Oxidation of 2-Heterocyclic BMIDAs

The synthesis of functionalized oxindoles and benzofuranones via oxidation of 2-BMIDA indoles and benzofurans, respectively, is described. Interconversion of boron species (BMIDA→BF3K) was necessary to enable oxidation and overcome boronic acid stability issues associated with a difficult BMIDA hydrolysis. Overall, a robust process was developed that allowed access to a small library of oxindole and benzofuranone products and facilitated the step-efficient synthesis of biologically active compounds containing the oxindole pharmaco-phore.