79563-56-7

Upstream product

• 42516-28-9 ethyl (2E)-4-(diethoxyphosphoryl)crotonate 
• 10236-14-3 4-(diethoxyphosphoryl)-but-2-enoic acid ethyl ester 
• 13991-36-1 4-bromocrotonic acid 
• 122-52-1 triethyl phosphite 
• 67629-62-3 methyl 4-(diethylphosphono)crotonate 
• 1067-87-4 Diethyl allylphosphonate 
• 124-38-9 carbon dioxide 

Downstream Products

• 124944-55-4 {(E)-3-[[(E)-(1S,7S)-9-[(3S,5R)-5-((Z)-3-Hydroxy-2-methyl-propenyl)-2,3-dimethoxy-cyclopent-1-enyl]-7-(4-methoxy-benzyloxy)-9-oxo-1-phenyl-non-3-enyl]-(4-methoxy-benzyl)-carbamoyl]-allyl}-phosphonic acid diethyl ester 
• 124944-56-5 {(E)-3-[[(E)-(1S,7S)-9-[(3S,5R)-2,3-Dimethoxy-5-((Z)-2-methyl-3-oxo-propenyl)-cyclopent-1-enyl]-7-(4-methoxy-benzyloxy)-9-oxo-1-phenyl-non-3-enyl]-(4-methoxy-benzyl)-carbamoyl]-allyl}-phosphonic acid diethyl ester 

Relevant academic research and scientific papers

Synthesis of 2,3-dihydroxy-3-(N-substituted carbamoyl)propylphosphonic acid derivatives as hybrid DOXP-fosmidomycin analogues

A six-step synthetic pathway has been established to access a series of racemic 2,3-dihydroxy-3-(N-substituted carbamoyl)propylphosphonic acid derivatives, designed to contain structural features common to both the natural substrate 1-deoxy-D-xylulose 5-p

(2E,4E)-5-PHENYL-PENTA-2,4-DIEN-1-ONE DERIVATIVE

The present application relates to a novel pentadienoyl compound and a pharmaceutical composition including the same. The pentadienoyl compound of the present application may be used to prevent or treat fatty liver and fatty liver-related disease by inhibiting lipogenesis and lipid accumulation in cells and activating lipid metabolism. In addition, the pentadienoyl compound of the present application may increase a SIRT1 expression level in cells or SIRT1 activity, and thus may be used to prevent or treat a SIRT1-mediated disease. In addition, the pentadienoyl compound of the present application may reduce a CK2 expression level in cells or CK2 activity, and thus may be used to prevent or treat a CK2-mediated disease.

Total Synthesis of the Endocannabinoid Uptake Inhibitor Guineensine and SAR Studies

Guineensine ((2E,4E,12E)-13-(benzo[d][1,3]dioxol-5-yl)-N-isobutyltrideca-2,4,12-trienamide) is a plant-derived natural product that inhibits reuptake of the endocannabinoid anandamide with sub-micromolar potency. We have established a highly efficient tot

Total Synthesis of δ-Sanshool and Analogues Thereof

Two simple synthetic approaches were developed for the total synthesis of δ-sanshool, an isobutylamide characterized by a C14 pentaunsaturated chain with all trans double bonds and proposed as a promising lead for the treatment of type-1 diabetes due to its dual activity on cannabinoid (CB) receptors. The syntheses are based on a suitably protected core fragment derived from 1,4-butanediol. These strategies also enable the preparation of small libraries of chemical analogues modified at either the polyunsaturated alkyl chain or the amidic head for use in SAR studies.

NOVEL PIPERINE DERIVATIVES AND USES THEREOF

The present invention provides novel piperine derivatives. The present pharmaceutical or food composition containing a piperine derivative as an active ingredient is very effective in preventing or treating metabolic diseases including obesity, diabetes, dyslipidemia, fatty liver and insulin resistance syndrome. Piperine derivatives of the present invention useful as pharmaceuticals compositions or functional food compositions has therapeutic efficacies for metabolic syndrome selected from the group consisting of obesity, diabetes, hyperlipidemia, fatty liver and insulin resistance syndrome, and also suppress the differentiation of progenitor cells and reduce the accumulation of triglycerides.

NOVEL PIPERINE DERIVATIVE AND USE THEREFOR

The present invention provides novel piperine derivatives. The present pharmaceutical or food composition containing a piperine derivative as an active ingredient is very effective in preventing or treating metabolic diseases including obesity, diabetes,

METHOD FOR PRODUCING SANSHOOL

Provided are a method for producing a sanshool, which can produce a sanshool in a short process and with high stereoselectivity, as well as a novel diene iron complex compound that is a stable intermediate useful for the production method. The diene iron complex compound is represented by the following general formula (I): (in which A represents CO, P(RA)3, CN, NO, SO(RA)3, or N(RA)2; RA represents a straight chain or branched chain alkyl group having 1 to 4 carbon atoms or an aryl group having 6 to 12 carbon atoms; and one of R1 and R2 represents a hydrogen atom and the other one thereof represents a structure represented by the following formula (II)): (in which R represents a hydrogen atom, a hydroxyl group, or a methyl group).

Application of iron carbonyl complexation to the selective total synthesis of sanshools

We focused on the iron-complexes of sanshools (hydroxyl-α-sanshool, hydroxyl-β-sanshool, and γ-sanshool) as the key intermediates for the selective synthesis of these structurally unstable compounds. Consequently, we developed a concise and selective method for the total synthesis of sanshools in 5-6 steps (26-45% overall yield), including complexation of dienes with iron tricarbonyl group.

Fixation of heterocumulenes, II. - A study on the reaction of lithiated allyl systems with CO2, isocyanates and isothiocyanates

The regioselectivity of the reaction of 1-(thiophenyl)- (Li-6), 1-(phenylsulfinyl)- (Li-12), 1-(phenylsulfonyl)- (Li-15) and 1-(diethoxyphosphoryl)allyllithium (Li-18) with CO2, PhNCO and PhNCS is investigated. Carboxylation of the allyl sulfide 6 and the allyl sulfoxide 12 proceeds with low regioselectivity. On the other hand, an exclusive γ-selectivity is achieved for reactions of CO2 with Li-15 and Li-18. Both carboxylations are reversible and can be directed to give a-products by using low temperature workup (0 °C). In contrast to CO2, PhNCO reacts with the allylic compounds investigated here to give amides with a high degree of regioselectivity: α-Attack is found for the sulfide 6 and the sulfone 15 whereas the reaction occurs at the γ-terminus for the sulfoxide 12 and the phosphonate 18. Exclusive α-attack is observed for all sulfur-substituted allyllithium compounds on reaction with PhNCS. In contrast to this, reaction of the phosphonate 18 with PhNCS yields exclusively the γ-product.

Synthesis of Substrate Analogues and Inhibitors for the Phosphoglycerate Mutase Enzyme

Several substrate analogues of the title enzyme were synthesized as well as with possible irreversible inhibitors, analogues of phosphoglycolate, the cofactor for this enzyme.The main routes involved an Arbuzov type reaction on functionalized halides, a reaction significantly improved by a sonication procedure and reaction of the diethylphosphite anion on tosylates.Phosphorylated epoxides were obtained by quantitative oxidation of conjugate double bonds using DMDO.Preliminary assays indicated a promising activity in some of these compounds.Keywords: phosphonates; inhibitors; phosphoglycerate Mutase; Arbuzov; DMDO