51816-46-7

Upstream product

• 103-25-3 3-phenylpropanoic acid methyl ester 
• 141-43-5 ethanolamine 
• 65-85-0 benzoic acid 
• 107978-04-1 3-(1-oxo-3-phenylpropyl)-1,3-oxazolidin-2-one 
• 109318-10-7 2,5-dioxopyrrolidin-1-yl 3-phenylpropanoate 
• 104-53-0 3-phenyl-propionaldehyde 
• 91564-20-4 N-(2-hydroxypropyl)-3-phenylpropanamide 
• 20627-49-0 3-phenyl-propionic acid butyl ester 
• 1178001-75-6 (S)-N-(1-hydroxypropan-2-yl)-3-phenylpropanamide 
• 401587-50-6 N-(3-hydroxypropyl)-3-phenylpropanamide 
• 501-52-0 3-Phenylpropionic acid 
• 645-45-4 hydrocinnamic acid chloride 

Downstream Products

• 51816-10-5 N-(2-chloro-ethyl)-3-phenyl-propionamide 
• 51816-21-8 2-(2-phenylethyl)-Δ²-oxazoline 
• 13326-06-2 n-propyl 3-phenylpropionate 
• 2021-28-5 ethyl dihydrocinnamate 
• 232949-65-4 pentyl 3-phenylpropionoate 
• 20627-49-0 3-phenyl-propionic acid butyl ester 

Relevant academic research and scientific papers

Ammonia-borane as a Catalyst for the Direct Amidation of Carboxylic Acids

Ammonia-borane serves as an efficient substoichiometric (10%) precatalyst for the direct amidation of both aromatic and aliphatic carboxylic acids. In situ generation of amine-boranes precedes the amidation and, unlike the amidation with stoichiometric amine-boranes, this process is facile with 1 equiv of the acid. This methodology has high functional group tolerance and chromatography-free purification but is not amenable for esterification. The latter feature has been exploited to prepare hydroxyl- and thiol-containing amides.

Broadly Applicable Ytterbium-Catalyzed Esterification, Hydrolysis, and Amidation of Imides

An efficient, broadly applicable, operationally simple, and divergent process for the transformation of imides into a range of carboxylic acid derivatives under mild conditions is reported. By simply using catalytic amounts of ytterbium(III) triflate as a Lewis acid promoter in the presence of alcohols, water, amines, or N,O-dimethylhydroxylamine, a broad range of imides is smoothly and readily converted to the corresponding esters, carboxylic acids, amides, and Weinreb amides in good yields. This method notably enables an easy cleavage of oxazolidinone-based auxiliaries.

Compounds with cardiac myosin activating function and pharmaceutical composition containing the same for treating or preventing heart failure

The present invention relates to a compound having a cardiotonic activating function and a pharmaceutical composition containing the same. The composition comprising the compound according to the present invention is effective in preventing or treating heart failure. In addition, the compound is represented by chemical formula 2 or is pharmaceutically acceptable salt thereof.COPYRIGHT KIPO 2016

Compounds with cardiac myosin activating function and pharmaceutical composition containing the same for treating or preventing heart failure

Disclosed are a compound having cardiotonic activity and a pharmaceutical composition containing the same, and the composition containing the compound, according to the present invention, is useful for preventing and treating heart failure.COPYRIGHT KIPO 2016

Metal-free oxidative amide formation with N-hydroxysuccinimide and hypervalent iodine reagents

An oxidative amide formation using N-hydroxysuccinimide and hypervalent iodine reagents was developed. The method enables a wide range of aldehydes and amines to be coupled under mild reaction conditions providing amide in good to excellent yield. The radical species in the reaction mixture was observed for the first time using ESR measurement, and along with other mechanistic investigations, a plausible mechanism of the reaction was proposed.

Enzymatic synthesis of N-acylethanolamines: Direct method for the aminolysis of esters

Immobilized Candida antarctica (Novozyme 435) catalyzed synthesis of N-acylethanolamines is described. Treatment of methyl esters with lipase and amines yielded the desired amides within 2-24 h with yields ranging from 41% to 98%.

Zinc-catalyzed amide cleavage and esterification of β- hydroxyethylamides

Snipping tool: Zn(OTf)2 is an efficient catalyst for selective cleavage of amides bearing a β-hydroxyethyl group on the nitrogen atom. The mechanism involves an N,O-acyl rearrangement and transesterification. This new catalytic system can be applied to sequence-specific peptide bond scission at the amine side of a serine residue. Tf=trifluoromethanesulfonyl. Copyright

Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives

A series of novel N-(2-hydroxyethyl) cinnamamide derivatives were synthesized and screened for their anticonvulsant activities by the maximal electroshock (MES) test and their neurotoxicity was evaluated by the rotarod neurotoxicity test (Tox). The MES test showed that compounds I(N-(2-hydroxyethyl) cinnamamide) and 1d ((E)-3-(3-fluorophenyl)-N-(2-hydroxyethyl)acrylamide) were found to possess better anticonvulsant activity but also had lower toxicity. In the anti-MES potency test, these compounds exhibited median effective dose (ED50) of 17.7 and 17.0 mg/kg, respectively, and median toxicity dose (TD50) of 154.9 and 211.1, respectively, resulting in a protective index (PI) of 8.8 and 12.4, respectively, which is much greater than the PI of the marked antiepileptic drug carbamazepine. To further investigate the effects of the anticonvulsant activity in several different models, compounds I and 1d were tested against convulsions induced by chemical substances, including pentylenetetrazole (PTZ), isoniazid, 3-mercaptopropionic acid, and thiosemicarbazide.

Development of chlorotriazine polymer dehydrocondensing reagents (Poly-Trzs)

Polymer-type dehydrocondensing reagents comprising of a triazine dehydrocondensing reagent, itself in a polymerized form (Poly-Trz-MMs'), have been developed by exploiting the chemical properties of cyanuric chloride that readily binds to alcohol or amines. A chlorotriazine polymer bearing two alkoxy substituents at the 4- and 6- positions (Poly-O-Trz-Cl) was prepared by alternating copolymerization between cyanuric chloride and tetra(ethylene glycol). Similarly, polymers bearing both alkoxy and amino substituents (Poly-N-Trz-Cl) were synthesized from tetra(ethylene glycol) bis(4,6-dichlorotriazin-2-yl) ether 6 and tris(2-aminoethyl)amine 7 and/or ethylenediamine 8. All the polymers were shown to be good reagents for dehydrocondensation of carboxylic acids and amines in the presence of NMM, compared to the corresponding monomeric dehydrocondensing reagent (DMT-MM). The advantages of the polymeric reagents are as follows: (1) both the reaction and isolation procedure of dehydrocondensation can be greatly simplified, (2) the dehydrocondensation can be conducted in protic solvents as well as in common organic solvents, (3) the reagents can be efficiently prepared at a low cost, and (4) these reagents are considered eco-friendly, generating a lower amount of waste compared to conventionally related reagents because of high loading of the dehydrocondensing activity (ca. 3 mequiv/g).

METHOD AND APPARATUS FOR THE USE OF [11C] CARBON MONIXIDE IN LABELING SYNTHESIS BY PHOTO-INITIATED CARBONYLATION

Methods and reagents for photo-initiated carbonylation with carbon-isotope labeled carbon monoxide using amines and alkyl/aryl iodides are provided. The resultant carbon-isotope labeled amides are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.