4025-75-6

Usage

Uses

Used in Pharmaceutical Industry:
(4-Nitrophenyl)methanesulfonyl chloride is used as a reagent for the preparation of HIV-1 Tat protein. This is achieved through native chemical ligation between a peptide thioester and a peptide containing (mercapto)leucine at the N-terminus, followed by desulfurization. This process plays a crucial role in the development of therapeutic strategies against HIV.

InChI:InChI=1/C7H6ClNO4S/c8-14(12,13)5-6-1-3-7(4-2-6)9(10)11/h1-4H,5H2

Upstream product

• 13287-49-5 4-Nitro-benzylthiocyanat 
• 53992-33-9 (4-nitrophenyl)-methanesulfonic acid 
• 39549-05-8 bis(4-nitrobenzyl)disulfide 
• 36639-50-6 Sodium 4-nitrobenzylsulphonate 
• 71-23-8 propan-1-ol 
• 56-23-5 tetrachloromethane 
• 7782-50-5 chlorine 
• 64-17-5 ethanol 
• 4357-96-4 S-(4-nitro-benzyl)-isothiourea; hydrochloride 
• 170640-75-2 S-(4-nitrophenylmethyl)thioacetate 
• 100-87-8 Benzylsulfonic acid 
• 10026-13-8 phosphorus pentachloride 
• 64039-36-7 S-(4-nitrobenzyl)isothiourea hydrobromide 
• 100-14-1 4-nitrobenzyl chloride 

Downstream Products

• 61801-10-3 (4-Nitro-phenyl)-methanesulfonic acid 4-(4-nitro-phenylmethanesulfonyloxy)-butyl ester 
• 110661-61-5 (p-nitrophenyl)methanesulfonyl fluoride 
• 53992-31-7 C-(4-nitrophenyl)-N-phenylmethanesulfonamide 
• 85650-20-0 (4-Nitro-phenyl)-methanesulfonic acid 2-chloro-ethyl ester 
• 53992-04-4 Phenyl-p-nitro-phenylmethan-sulfonat 
• 100-14-1 4-nitrobenzyl chloride 
• 56157-83-6 (4-Nitro-phenyl)-methanesulfonic acid 2,4-dinitro-phenyl ester 
• 10602-28-5 C₈H₈⁽²⁾HNO₅S 
• 85260-63-5 Trimethyl-[(E)-2-(4-nitro-phenyl)-vinyl]-silane 
• 736-31-2 trans-4,4'-dinitrostilbene 
• 88918-72-3 4-nitrobenzenemethanesulphonamide 
• 803727-91-5 N,N-bis(2,4-dimethoxybenzyl)-1-(4-nitrophenyl)methanesulfonamide 
• 939403-25-5 dimethyl 2-{[methoxy(2-methyl-1-{[(4-nitrobenzyl)sulfonyl]amino}propyl)phosphoryl]methyl}pentanedioate 
• 939403-26-6 dimethyl 2-{[methoxy(2-methyl-1-{[(4-nitrobenzyl)sulfonyl]amino}butyl)phosphoryl]methyl}pentanedioate 

Relevant academic research and scientific papers

Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγInverse Agonist for Treatment of Castration-Resistant Prostate Cancer

We report the design, optimization, and biological evaluation of nuclear receptor RORγinverse agonists as therapeutic agents for prostate cancer treatment. The most potent compound 27 (designated as XY101) exhibited cellular activity with an IC50/su

Olefination with Sulfonyl Halides and Esters: E-Selective Synthesis of Alkenes from Semistabilized Carbanion Precursors

Carbanions of sulfonyl halides and activated sulfonates add to carbonyl compounds, and so-formed aldol-type adducts spontaneously fragment into olefins. This transformation mimics the one-pot Julia olefination with (hetero)aryl sulfones, but the mechanism of fragmentation involves a four-membered intermediate, typical for reactivity of phosphorus reagents. Moreover, in contrast to the reactions of sulfones, sulfonates of fluorinated alcohols (TFE and HFI) produce byproducts that are easily removed during workup. In our report, we focus on reactions of unstabilized and semistabilized carbanion precursors: alkylsulfonates, and allyl- and benzylsulfonates, respectively. In particular for semistabilized systems, olefins were synthesized as predominant E isomers in good yields. The presented studies reveal that optimal reaction conditions, including the type of base and alcohol groups of the sulfonates, are different depending on stabilization of the carbanion precursors and structure of the carbonyl substrates. The practical synthetic guide is supplemented with a discussion of the mechanism, based on reactivity studies of intermediates and identification of side-products.

Preparation method of almotriptan key intermediate 1-(4-amino-phenylmethylsulfonyl)pyrrolidine

The invention discloses a preparation method of an almotriptan key intermediate 1-(4-amino-phenylmethylsulfonyl)pyrrolidine. The main steps comprise: 1) preparing a Vilsmeier reagent by using BTC andDMF, and carrying out a sulfonylation reaction on p-nitr

Tert -Butyl Hypochlorite Mediated Oxidative Chlorination of S -Alkylisothiourea Salts: Synthesis of Sulfonyl Chlorides

Under neutral conditions, a variety of S-alkylisothiourea salts were smoothly converted into the corresponding sulfonyl chlorides through tert-butyl chlorite mediated oxidative chlorination in good to excellent yields after simple purification. In addition to the environmental and procedural advantages of this method, the neutral conditions potentially make it applicable to substrates that bear acid-sensitive functional groups. For example, the Cbz-protected 2-aminoethanesulfonyl chloride could be synthesized in moderate to good yields under the current neutral conditions, and the acid-sensitive Cbz-protecting group was not affected.

Clean and economic synthesis of alkanesulfonyl chlorides from S-alkyl isothiourea salts via bleach oxidative chlorosulfonation

A simple procedure for clean and economic synthesis of alkanesulfonyl chlorides via bleach-mediated oxidative chlorosulfonation of S-alkyl isothiourea salts is disclosed. This procedure is environment- and worker-friendly with the advantages of readily accessible materials and reagents, simple and safe operations, easy purification without chromatography, and affords high yields of up to 99%.

Simple synthesis of sulfonyl chlorides from thiol precursors and derivatives by NaClO2-mediated oxidative chlorosulfonation

A simple method to synthesize diverse sulfonyl chlorides through NaClO 2-mediated oxidative chlorosulfonation of S-alkyl isothiourea salts is presented. The approach features safe operation, environmental friendliness, convenient purification procedures, and delivers high yields of up to 96%. The procedure is also applicable to substrates such as thiols, disulfides, thioacetates, and xanthates. It is a versatile and convenient method for the synthesis of various sulfonyl chlorides from different thiol precursors and derivatives. Georg Thieme Verlag Stuttgart, New York.

INDOLYLALKYL DERIVATIVES OF PYRIMIDINYLPIPERAZINE AND METABOLITES THEREOF FOR TREATMENT OF ANXIETY, DEPRESSION, AND SEXUAL DYSFUNCTION

The present invention relates to a method for alleviation, prevention, and treatment of anxiety, depression, and sexual dysfunction by administering certain indolylalkyl derivatives of pyrimidinylpiperazine or metabolites thereof. A preferred embodiment is of the following formula:

PREPARATION AND UTILITY OF SUBSTITUTED INDOLES

Disclosed herein are substituted indoles of Formula I, processes of preparation there of, pharmaceutical compositions thereof, and methods of their use there of.

Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis

This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds in the treating or preventing thrombosis in a mammal, or preventing progression of symptoms of thrombosis.

Sulfonyl chloride formation from thiol derivatives by N-chlorosuccinimide mediated oxidation

Oxidation of several thiol derivatives by a combination of N-chlorosuccinimide and dilute hydrochloric acid proceeded smoothly, affording the corresponding sulfonyl chlorides in good yield. Georg Thieme Verlag Stuttgart.