32617-55-3

Upstream product

• 112970-56-6 N-(4-chloro-2-vinylphenyl)-4-methylbenzenesulfonamide 
• 17422-32-1 5-chloro-1H-indole 
• 98-59-9 p-toluenesulfonyl chloride 
• 112970-51-1 N-(2-bromo-4-chlorophenyl)-4-methylbenzenesulfonamide 
• 1123-84-8 2,5-dichlorostyrene 
• 127-65-1 chloroamine-T 
• 1616975-00-8 N-(4-chloro-2-ethynylphenyl)-4-methylbenzenesulfonamide 
• 99448-80-3 5-chloro-1-tosylindoline-2,3-dione 
• 17630-76-1 5-chloroindole 2,3-dione 
• 873-38-1 4-chloro-2-bromoaniline 
• 143261-97-6 2-(1-isopropylthio-2-methoxyethyl)-4-chloroaniline 
• 106-47-8 4-chloro-aniline 
• 402822-77-9 N-allyl-N-p-toluenesulfonyl-4-chloro-2-ethenylaniline 
• 143262-01-5 N-tosyl-2-(1-isopropylthio-2-methoxyethyl)-4-chloroanilide 

Downstream Products

• 17422-32-1 5-chloro-1H-indole 
• 1579268-76-0 N-(3-(5-chloro-1-tosyl-1H-indol-2-yl)-3-hydroxypropyl)-N-(4-methoxybenzyl)-4-methylbenzenesulfonamide 
• 1579269-00-3 9-chloro-5-(4-methoxyphenyl)-2,6-ditosyl-1,2,3,4,5,6-hexahydroazepino[4,3-b]indole 
• 112398-75-1 5-chloro-1-methyl-1H-indole 

Relevant academic research and scientific papers

A Series of 2-((1-Phenyl-1H-imidazol-5-yl)methyl)-1H-indoles as Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors

Indoleamine 2,3-dioxygenase 1 (IDO1) is a promising therapeutic target in cancer immunotherapy and neurological disease. Thus, searching for highly active inhibitors for use in human cancers is now a focus of widespread research and development efforts. I

Design, Synthesis, and Antifungal Evaluation of Cryptolepine Derivatives against Phytopathogenic Fungi

Inspired by the widely antiphytopathogenic application of diversified derivatives from natural sources, cryptolepine and its derivatives were subsequently designed, synthesized, and evaluated for their antifungal activities against four agriculturally important fungi Rhizoctonia solani, Botrytis cinerea, Fusarium graminearum, and Sclerotinia sclerotiorum. The results obtained from in vitro assay indicated that compounds a1-a24 showed great fungicidal property against B. cinerea (EC50 4 μg/mL); especially, a3 presented significantly prominent inhibitory activity with an EC50 of 0.027 μg/mL. In the pursuit of further expanding the antifungal spectrum of cryptolepine, ring-opened compound f1 produced better activity with an EC50 of 3.632 μg/mL against R. solani and an EC50 of 5.599 μg/mL against F. graminearum. Furthermore, a3 was selected to be a candidate to investigate its preliminary antifungal mechanism to B. cinerea, revealing that not only spore germination was effectively inhibited and the normal physiological structure of mycelium was severely undermined but also detrimental reactive oxygen was obviously accumulated and the normal function of the nucleus was fairly disordered. Besides, in vivo curative experiment against B. cinerea found that the therapeutic action of a3 was comparable to that of the positive control azoxystrobin. These results suggested that compound a3 could be regarded as a novel and promising agent against B. cinerea for its valuable potency.

Silver-Catalyzed Asymmetric Dearomatization of Electron-Deficient Heteroarenes via Interrupted Barton–Zard Reaction

Herein we report a catalytic asymmetric dearomatization reaction of electron-deficient heteroarenes with α-substituted isocyanoacetates through an interrupted Barton–Zard reaction. A range of optically active pyrrolo[3,4-b]indole derivatives was obtained

A Catalytic Construction of Indoles via Formation of Ruthenium Vinylidene Species from N-Arylynamides

Treatment of ynamides with a catalytic amount of TpRuCl(PPh3)2 resulted in the construction of indole scaffolds known as privileged structure motifs. This reaction involved a cascade of 1,2-rearrangement and cyclization carrying out C?C bond formation via a ruthenium vinylidene intermediate, as revealed by a deuterium-labeling experiments. Furthermore, the transformation of multi-functionalized ynamide, derived from a practical drug molecule, showed a high functional group tolerance of this reaction. (Figure presented.).

Iodine-Mediated Electrochemical C(sp2)-H Amination: Switchable Synthesis of Indolines and Indoles

A metal-free electrochemical intramolecular C(sp2)-H amination using iodine as a mediator was developed. This method enables a switchable synthesis of indoline and indole derivatives, respectively, from easily available 2-vinyl anilines.

B(C6F5)3-Catalyzed Highly Chemoselective Reduction of Isatins: Synthesis of Indolin-3-ones and Indolines

A chemo- and site-selective reduction reaction of isatin derivatives using catalyst B(C6F5)3 and hydrosilanes is described. This transformation is operationally simple, proceeds under mild conditions, and is resistant to various functional groups. Thus, this efficient reaction using a combination of B(C6F5)3 and BnMe2SiH or B(C6F5)3 and Et2SiH2 could potentially be utilized to produce various indolin-3-ones and indolines, without the need for multistep procedures and metal catalysis conditions.

Electron Transfer Photoredox Catalysis: Development of a Photoactivated Reductive Desulfonylation of an Aza-Heteroaromatic Ring

Herein, we report a protocol for desulfonylation of aza-heteroaromatic rings via photoinduced electron transfer and hydrogen atom transfer. This general protocol has a wide substrate range and moderate to good yields. The utility of the method was demonstrated by the chemoselective desulfonylation of a molecule containing both an aliphatic and an aromatic sulfonamide. (Figure presented.).

Indole structure-containing compound or pharmaceutically acceptable salt, preparation method and application thereof

The invention discloses an indole structure-containing compound with a structure as shown in a general formula (I) or pharmaceutically acceptable salt, a preparation method and application thereof. The indole structure-containing compound or the pharmaceu

Practical and Scalable Synthesis of Borylated Heterocycles Using Bench-Stable Precursors of Metal-Free Lewis Pair Catalysts

A practical and scalable metal-free catalytic method for the borylation and borylative dearomatization of heteroarenes has been developed. This synthetic method uses inexpensive and conveniently synthesizable bench-stable precatalysts of the form 1-NHR2-2-BF3-C6H4, commercially and synthetically accessible heteroarenes as substrates, and pinacolborane as the borylation reagent. The preparation of several borylated heterocycles on 2 and 50 g scales was achieved under solvent-free conditions without the use of Schlenk techniques or a glovebox. A kilogram-scale borylation of one of the heteroarene substrates was also achieved using this cost-effective green methodology to exemplify the fact that our methodology can be conveniently implemented in fine chemical industries.

NOVEL NICOTINAMIDE DERIVATIVES OR SALTS THEREOF

An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. Th e present invention provides a nicotinamide derivative represented by the follo wing formula (I) (wherein R 1 represents a halogen atom; R 2 represents a C 1-12 alkyl group, a C 2-12 alkenyl group, a C 2-12 alkynyl group, a C 3-8 cycloalkyl g roup, an aryl group, an ar-C 1-6 alkyl group or a heterocyclic group, each opti onally having at least one substituent; R 3 represents an aryl group or a hetero cyclic group each optionally having at least one substituent; and R 4 and R 5 e ach independently represent a hydrogen atom; and R 2 and R 4 may form a cyc lic amino group optionally having at least one substituent together with the ni trogen atom to which they bind) or a salt thereof, and a pharmaceutical comp osition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.