3266-71-5

Upstream product

• 136-95-8 2-amino-benzthiazole 
• 98-88-4 benzoyl chloride 
• 84634-94-6 benzoylcyanamide calcium salt 
• 95-55-6 2-amino-phenol 
• 21406-30-4 N-Benzoylamino-dithiokohlensaeuremethylester 
• 23432-93-1 3-chloro-5-phenyl-1,2,4-oxadiazole 
• 4921-82-8 1-benzoyl-3-phenylthiourea 
• 4570-41-6 1,3-benzoxazol-2-amine 
• 65-85-0 benzoic acid 
• 591-50-4 iodobenzene 
• 201230-82-2 carbon monoxide 
• 139-02-6 sodium phenoxide 
• 24786-18-3 dimethyl N-benzoyldithiocarbonimidate 
• 120811-59-8 3-phenoxy-5-phenyl-1,2,4-oxadiazole 

Relevant academic research and scientific papers

Design, synthesis, and evaluation of substituted 2-acylamide-1,3-benzo[d]zole analogues as agents against MDR- and XDR-MTB

N-(5-Chlorobenzo[d]oxazol-2-yl)-4-methyl-1,2,3-thiadiazole-5-carboxamideox-amide has been identified as a potent inhibitor of Mtb H37Rv, with a minimum inhibitory concentration (MIC) of 0.42 μM. In this study, a series of substituted 2-acylamide-1,3-zole analogues were designed and synthesized, and their anti-Mtb activities were analyzed. In total, 17 compounds were found to be potent anti-Mtb agents, especially against the MDR- and XDR-MTB strains, with MIC values 10 μM. These analogues can inhibit both drug-sensitive and drug-resistant Mtb. Four representative compounds were selected for further profiling, and the results indicate that compound 18 is acceptably safe and has favorable pharmacokinetic (PK) properties. In addition, this compound displays potent activity against Gram-positive bacteria, with MIC values in the range of 1.48–11.86 μM. The data obtained herein suggest that promising anti-Mtb candidates may be developed via structural modification, and that further research is needed to explore other compounds.

2-Aminobenzimidazole and -benzoxazole as N-nucleophile in palladium-catalysed aminocarbonylation

Palladium-catalysed aminocarbonylation of aryl iodides in the presence of 2-aminobenzimidazole and 2-aminobenzoxazole as N-nucleophile was carried out. Single CO insertion took place, however, instead of the expected carboxamides (C(O)NH) the correspondin

Synthesis method of N-heterocyclic acylamide derivative

The invention discloses a synthesis method of an N-heterocyclic acylamide derivative. A reaction general formula is as shown in the specification. According to the synthesis method, an imidazo heterocyclic amine compound I is taken as a raw material; unde

Diacetoxyiodobenzene assisted C-O bond formation: Via sequential acylation and deacylation process: Synthesis of benzoxazole amides and their mechanistic study by DFT

An efficient method for the transformation of N-substituted-N′-benzoylthioureas to substituted N-benzoxazol-2-yl-amides using diacetoxyiodobenzene (DIB) is described in this work. The transformation follows the C-O bond formation leading to the benzoxazole derivative, due to oxidative dehydrogenation by DIB, instead of the expected C-S bond formation of the benzothiazole moiety. The C-O bond formation leading to benzoxazole is due to consecutive acylation and deacylation in conjunction with the reduction of two moles of DIB. A plausible mechanism was proposed for the reaction and density functional calculations were also performed to study the reaction mechanism.

An efficient solid-phase parallel synthesis of 2-amino and 2-amidobenzo[d]oxazole derivatives via cyclization reactions of 2-hydroxyphenylthiourea resin

An efficient solid-phase methodology has been developed for the synthesis of 2-amino and 2-amidobenzo[d]- oxazole derivatives. The key step in this procedure involves the preparation of polymer-bound 2-aminobenzo- [d]oxazole resins 4 by cyclization reaction of 2-hydroxyphenylthiourea resin 3. The resin-bound 2-hydroxyphenylthiourea 3 is produced by the addition of 2-aminophenol to the isothiocyanate-terminated resin 2 and serve as a key intermediate for the linker resin. This core skeleton 2-aminobenzo[d]oxazole resin 4 undergoes functionalization reaction with various electrophiles, such as alkylhalides and acid chlorides to generate 2- amino and 2-amidobenzo[d]oxazole resins 5 and 6 respectively. Finally, 2-amino and 2-amidobenzo[d]oxazole derivatives 7 and 8 are then generated in good yields and purities by cleavage of the respective resins 5 and 6 under trifluoroacetic acid (TFA) in dichloromethane (CH2Cl2).

Synthesis of benzoxazole amides as novel antifungal agents against Malassezia furfur

Malassezia is a pathogenic fungus that causes skin diseases, such as tinea versicolor, atopic dermatitis and fatal sepsis. We report the synthesis of a series of benzoxazole amides and evaluation of their antifungal activity against Malassezia furfur. Twe

Heterocyclic Photorearrangements. Photoinduced Rearrangements of 1,2,4,-Oxadiazoles Substituted by an XYZ Side Chain Sequence

Photoinduced rearrangements of 1,2,4-oxadiazoles substituted by an XYZ side chain sequence at position 3 of the ring have been recognized.Examples taken out from previous results have been emphasized and some other patterns dealing with a 3-phenoxy and 3-

Reactions with N-Acylimino-dithiocarbonic-acid-diesters

Reactions of N-acylimino-dithiocarbonic-acid-S,S-diesters 1 with nucleophilic compounds present new possibilities to synthesize heterocycles.With amines 1a reacts by mono- and disubstitution, respectively, of methylthio-groups to isothioureas 2 and guanidines 3, with 1,2-binucleophilic arenes to benzoheterocycles 4, with aliphatic diamines to imidazolines 5, pyrimidines 6, diazepines 7 and the hexamethylene-diamine-derivatives 8. 1a reacts also with hydrazines to 1,2,4-triazoles 9 and with hydrazides to the thiosemicarbazones 10 or 1,3,4-oxadiazoles 11.Heterocyclisations of 1 with guanidines, thiourea, salts of thiourea and amidines give the 1,3,5-triazines 12, 14, 15 and 16.N-benzoyl-dithiocarbonic-acid-methylester -amid reacts with CH-acidic compounds to thiazoles 17.The structures of the final products are determined by i.r.-, 1H-n.m.r.-, u.v.- and mass-spectras.