82745-22-0

Upstream product

• 17599-61-0 N-benzylidene-1,1,1-trimethylsilanamine 
• 18295-60-8 allenylmagnesium bromide 
• 22665-30-1 allenylzinc bromide 
• 780-25-6 N-benzylidene benzylamine 
• 624-65-7 2-propynyl chloride 
• 106-96-7 propargyl bromide 
• 107590-86-3 N-diphenylmethylene(1-phenyl-3-butynyl)amine 
• 7699-79-8 benzhydrylidene-benzyl-amine 
• 1192966-53-2 tert-butyl (1-phenylbut-3-yn-1-yl)carbamate 
• 100-52-7 benzaldehyde 
• 865350-17-0 4,4,5,5-tetramethyl-2-(propa-1,2-dien-1-yl)-1,3,2-dioxaborolane 
• 622-79-7 benzyl azide 
• 18295-60-8 propargyl magnesium bromide 
• 40963-57-3 2-Propynylzinc bromide 

Downstream Products

• 1192966-57-6 1-(2-chloroethyl)-3-(1-phenylbut-3-ynyl)urea 
• 1261217-91-7 N-(1-phenylbut-3-ynyl)pivalamide 
• 1261217-89-3 N-(1-phenylbut-3-ynyl)acetamide 
• 1261217-90-6 N-(1-phenylbut-3-ynyl)isobutyramide 
• 1262027-89-3 4-[(1-phenyl-3-butynyl)amino]quinazoline 
• 1262027-90-6 4-[(1,4-diphenyl-3-butynyl)amino]quinazoline 
• 285565-39-1 4-methyl-N-(1-phenylbut-3-yn-1-yl)benzenesulfonamide 

Relevant academic research and scientific papers

Silver-Catalyzed Three-Component 1,1-Aminoacylation of Homopropargylamines: α-Additions for Both Terminal Alkynes and Isocyanides

The reaction of secondary homopropargylamines, isocyanides, and water in the presence of a catalytic amount of silver acetate and subsequent purification by chromatography on silica gel afforded substituted proline amides in good to excellent yields. Primary homopropargylamines underwent a cyclizative Ugi–Joullié three-component reaction with isocyanides and carboxylic acids to afford functionalized N-acyl proline amides. High diastereoselectivity was observed in the synthesis of 4-alkoxy and 4,5-disubstituted proline derivatives. This work represents the first examples of a three-component cyclizative 1,1-aminoacylation of terminal alkynes.

Fragment-Based Drug Design Facilitated by Protein-Templated Click Chemistry: Fragment Linking and Optimization of Inhibitors of the Aspartic Protease Endothiapepsin

There is an urgent need for the development of efficient methodologies that accelerate drug discovery. We demonstrate that the strategic combination of fragment linking/optimization and protein-templated click chemistry is an efficient and powerful method that accelerates the hit-identification process for the aspartic protease endothiapepsin. The best binder, which inhibits endothiapepsin with an IC50value of 43 μm, represents the first example of triazole-based inhibitors of endothiapepsin. Our strategy could find application on a whole range of drug targets.

New enolate-carbodiimide rearrangement in the concise synthesis of 6-amino-2,3-dihydro-4-pyridinones from homoallylamines

Three-step synthesis of 6-amino-2,3-dihydro-4-pyridinones from homoallylamines involving NBS-mediated cyclization of N-(3-butenyl)ureas to 6-(bromomethyl)-2-iminourethanes, dehydrohalogenation and a novel rearrangement as a key step has been developed. Th

A Ru-catalyzed one-pot synthesis of homopropargylic amines from alkyl azides under photolytic conditions

A new synthetic method for homopropargylic amines from alkyl azides is presented. A salient feature of this reaction is the involvement of N-unsubstituted imines as the key intermediates, which are generated from alkyl azides by Ru catalysis under photoly

Agri-Horticultural Pest Control Compositions Comprising 4-(3-Butynyl)Aminopyrimidine Derivatives

Agri-horticultural pest control compositions having outstanding control effect on pests, in particular, agri-horticultural pests, which comprise as active ingredients one or more 4-(3-butynyl)aminopyrimidine derivatives represented by the general formula [I], namely, where R1 is typically selected from among: a) phenyl c) —SiR5R6R7 (R5, R6, and R7 which may be the same or different represent a linear or branched alkyl having 1-6 carbon atoms, a linear or branched haloalkyl having 1-3 carbon atoms which is substituted by one halogen atom, a linear or branched cyanoalkyl having 1-3 carbon atoms which is substituted by one cyano group, and phenyl); d) hydropgen atom; R2 typically represents a hydrogen atom; R3 typically represents a hydrogen atom; R4 represents a hydrogen atom and one or more agri-horticultural pest control compounds selected from among agri-horticultural antimicrobial compounds, say, multi-site contact active compouns, nucleic acids synthesis inhibitory active compounds, mitosis and cell divesion inhibitory active compounds, and/or agri-horticultural insecticidal, miticidal or nematicidal compounds, say, acetylcholinesterase inhibitors, GABA-gated chloride antagonists, and sodium channel modulators. Since the 4-(3-butynyl)aminopyrimidine derivatives and the existing antimicrobial active compounds and/or insecticidal active compounds are used in admixture, the 4-(3-butynyl)aminopyrimidine derivatives which are useful as pest control agents, particularly as agri-horticultural pest control agents, need be used in smaller amounts and yet their antimicrobial or insecticidal activity can be improved.

4-(3-BUTYNYL)AMINOPYRIMIDINE DERIVATIVES AS PEST CONTROL AGENTS FOR AGRICULTURAL AND HORTICULTURAL USE

Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, -R, -OR, -C(O)OR, -C(O)NHR, -CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) -CO-O-, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.

ALPHA2B AND ALPHA2C AGONISTS

Described herein are compounds that can be useful as bioactive agents. More specifically, the compounds described herein can be useful as both α2B and α2C adrenergic agonists. Methods of synthesis and administration of the compounds are also disclosed.

Synthese en une etape par voie organometallique d'amines primaires β-acetyleniques α-ramifiees

The one-pot synthesis of α-branched β-alcynyl primary amines results from reaction between organometallic compounds, prepared from propargylic bromides and N-silylimines derived from aromatic or aliphatic aldehydes.Ususally, the reaction is regioselective

ALKYLATION OF SCHIFF BASES BY HALIDES OF THE PROPARGYL TYPE

The alkylation of N-diphenylmethylenebenzylamine with 3-bromo-1-propyne and 1-bromo-2-pentyne under the conditions of phase-transfer catalysis was investigated.It was established that the process takes place unambiguously, and the yield of the primary γ-a

ALKYLATION OF N-BENZYLIDENEBENZYLAMINE BY HALIDES OF THE PROPARGYL TYPE

The alkylation of N-benzylidenebenzylamine by halides of the propargyl type under the conditions of interphase catalysis was investigated.It was established that the yield of the γ-acetylenic amine 1-phenyl-1-amino-3-butyne under these conditions amounts to only 5-10 percent, while diphenylethylenediamine is formed with yields of 20-25 percent.Propargylation of N-benzylidenebenzylamine gives a satisfactory yield when the reaction is carried out through the preliminary stage of metallation with observance of the temperature conditions (-70 deg C).