173423-55-7

Upstream product

• 1570-95-2 2-phenylpropane-1, 3-diol 
• 18162-48-6 tert-butyldimethylsilyl chloride 
• 60-29-7 diethyl ether 
• 37434-59-6 dimethyl 2-phenylmalonate 

Downstream Products

• 219708-55-1 3-[3-(tert-Butyl-dimethyl-silanyloxy)-2-phenyl-propyl]-oxazolidine-2,4-dione 
• 6052-63-7 2-phenylbut-3-en-1-ol 
• 172223-20-0 methyl (+/-)-(2E)-5-hydroxy-4-phenyl-2-pentenoate 
• 173423-56-8 (+/-)-(3Z)-2-phenyl-3-penten-1-ol 
• 173423-60-4 (+/-)-1-(bromoacetyloxy)-2-phenyl-3-butene 
• 173423-61-5 (+/-)-(2Z)-1-(bromoacetoxy)-2-phenyl-3-pentene 
• 173423-57-9 (+/-)-1-(2'-bromo-1'-ethoxyethoxy)-2-phenyl-3-butene 
• 1027225-90-6 (E)-5-(tert-Butyl-dimethyl-silanyloxy)-4-phenyl-pent-2-enoic acid methyl ester 
• 173423-62-6 methyl (+/-)-(2E)-5-(bromoacetoxy)-4-phenyl-2-pentenoate 

Relevant academic research and scientific papers

Tuning Isonitrile/Tetrazine Chemistry for Accelerated Deprotection and Formation of Stable Conjugates

The isocyano group is a valuable functionality for bioorthogonal reactions because it rapidly reacts with tetrazines to either form stable conjugates or release payloads from 3-isocyanopropyl groups. Here we provide mechanistic insights into the dissociative steps that follow the initial cycloaddition and analyze how structural modifications affect these processes. Three main outcomes of this study have important implications for designing such groups for bioorthogonal applications. First, anion-stabilizing substituents at C-2 of the 3-isocyanopropyl group promote β-elimination and accelerate deprotection. Second, tetrazines with bulky substituents form stable imine conjugates even with primary isonitriles that are otherwise rapidly hydrolyzed. Third, the elimination step is independent from hydrolysis to the aldehyde and instead can occur directly from the imine intermediate. These findings will allow tuning the structures of tetrazine and isonitrile reactants for application in bioorthogonal ligation and release chemistry.

RAPIDLY RELEASED BIOORTHOGONAL CAGING GROUPS

Bioorthogonal molecules are disclosed and described. A bioorthogonal a molecule having a structure according to: Formula (I); where R2, R3, and R4 are independently selected from H, a substituted or unsubstituted C1/

TETRAHYDRO-IMIDAZO QUINOLINE COMPOSITIONS AS CBP/P300 INHIBITORS

The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.

FUSED [1,2,4]THIADIAZINE DERIVATIVES WHICH ACT AS KAT INHIBITORS OF THE MYST FAMILY

A compound of formula (I): which inhibits the activity of one or more KATs of the MYST family, i.e., TIP60, KAT6B, MOZ, HBO1 and MOF.

PYRAZOLE DERIVATIVE, OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF

[Problem] The present invention is to provide a novel pyrazole derivative, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and a pharmaceutical use thereof. [Solution] The present invention provides a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof, which has TRPM8 inhibitory effects: wherein ring A is C6-10 aryl or the like; X is CR4a or the like; R1 and R2 are a hydrogen atom or the like; R3 is a hydrogen atom or the like; R4 is a hydrogen atom or the like; ring B is C6-10 aryl or the like; R5 is a hydrogen atom or the like; R6a is a hydrogen atom or the like; R7a is a hydrogen atom or the like; R7b is a hydrogen atom or the like; R6b is a hydrogen atom or the like; R8 is a hydrogen atom or the like; n is 0, 1 or 2. Therefore, the compound represented by the formula (I) of the present invention or a pharmaceutically acceptable salt thereof is useful as an agent for treating or preventing diseases or symptoms caused by hyperexcitability or disorder of afferent neurons.

Method for producing pyrazole derivative

PROBLEM TO BE SOLVED: To provide a method for producing a pyrazole derivative. SOLUTION: There is provided the method for producing a pyrazole derivative by using a compound represented by formula (IIC), (IID) or (III) and a compound represented by formula (IV). SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT

CHOLESTERYL ESTER TRANSFER PROTEIN INHIBITORS

Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A1 is a cyclic group, and B is a cyclic group which is attached to the heterocyclic ring directly or through a methylene group.

SPIRO-SUBSTITUTED AZACYCLES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY

The present invention is directed to spiro-substituted azacycles of the Formula 1: STR1 (wherein R 1, l, m, Q, W, X, Y, and Z are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.

Diastereoselective synthesis of ω-phosphonic acid analogues of 4-arylkainoids

Radical cyclisation by the use of α,β-unsaturated phosphonate as a radical acceptor was applied to a synthesis of 7-phosphonomethylpyrrolo[1,2-c]oxazolidinones, synthetic intermediates on the route to phosphonic acid analogues of kainoids. The relative configuration at the 6;7;7a-positions was found to be highly controlled by steric effects due to the substituent at the 6-position. Thus, diethyl [{(6S*,7R*,7aS*)-6-(2-methoxyphenyl)-3-oxoperhydropyrrolo[1,2- c]-[1,3]oxazol-7-yl}methyl]phosphonate 29a and diethyl [{(6S*,7R*,7aS*)-3-oxo-6-phenylperhydropyrrolo[1,2-c][1,3]- oxazol-7-yl}methyl]phosphonate 29b were prepared with high diastereoselectivity. When the substituent at the 6-position is a 1-naphthyl group, the diethyl [{(6S*,7R*,7aS*)-6-(1-naphthyl)pyrroloxazol-7-yl}methyl] phosphonate 29c and its (6S*,7R*,7aR*)-isomer 30c were formed in the ratio 29c:30c～2:1. The stereostructure of compound 29a was determined by X-ray crystallographic analysis. The 6-o-methoxyphenyl derivative 29a was converted into the corresponding phosphonic acid analogue 33.

Influence of a 2-fluoro substituent on diastereoselectivity in the 1,3-dipolar cycloadditions of nitrones

It is clear that the role of 1,2-asymmetric induction on the 1,3-dipolar cycloaddition of nitrones is influenced by the presence of a fluorine atom at the C-2 position. 2-Fluoro nitrones, synthesized by three different methods, have been subjected to the intermolecular 1,3-dipolar cycloaddition with ethyl vinyl ether. The stereostructures of isoxazolidines formed were determined by their conversion into 2,7-dioxa-6-azabicyclo[3.2.1]octanes. The diastereoselectivity of 2-fluoro nitrones was the reverse of that of the corresponding 2-hydro nitrones. This fact supports that the conformation with relief from the dipole repulsion between the fluorine atom and the oxygen atom of the nitrone is a preferred one for 2-fluoro nitrones, while the corresponding 2-hydro nitrones adopt the conformation with the least 1,3-allylic strain.