618094-94-3

Upstream product

• 136918-14-4 phthalimide 
• 173423-55-7 3-((tert-butyldimethylsilyl)oxy)-2-phenylpropan-1-ol 
• 1570-95-2 2-phenylpropane-1, 3-diol 
• 18162-48-6 tert-butyldimethylsilyl chloride 

Downstream Products

• 62247-39-6 3-Hydroxy-2-phenyl-1-aminopropane 
• 677325-05-2 hexahydro-4-oxo-5-phenyl-3a,5-bis(phenylselanyl)furo[2,3-b]pyridine-7-carboxylic acid tert-butyl ester 
• 677325-01-8 [3-hydroxy-3-(tetrahydro-2-oxofuran-3-yl)-2-phenylpropyl]carbamic acid tert-butyl ester 
• 677325-02-9 [3-hydroxy-3-(tetrahydro-2-hydroxyfuran-3-yl)-2-phenylpropyl]carbamic acid tert-butyl ester 
• 677325-00-7 [3-[(tert-butyldimethylsilanyl)oxy]-2-phenylpropyl]carbamic acid tert-butyl ester 
• 677325-04-1 hexahydro-4-oxo-5-phenylfuro[2,3-b]pyridine-7-carboxylic acid tert-butyl ester 
• 677325-03-0 hexahydro-4-hydroxy-5-phenylfuro[2,3-b]pyridine-7-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

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/

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.

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.

Model Studies and First Synthesis of the Antifungal and Antibacterial Agent Cladobotryal

The antifungal and antibacterial agent cladobotryal (1) was synthesized by a convergent route from lactone 31 and aldehyde 13, a key step in the elaboration of the pyridinone ring being conversion of a Boc group on nitrogen into a CO2SiPr-i3 group. The simple model compounds 9 and 10, representing the core of cladobotryal and of 5, respectively, were prepared as support studies for making the natural product.

First synthesis of the antifungal and antibacterial agent cladobotryal

The antifungal and antibacterial agent cladobotryal (1) was synthesized by a convergent route from lactone 5 and aldehyde 12, a key step in the elaboration of the pyridinone ring being conversion of a t-BuOC(O) group on nitrogen into an i-Pr3SiOC(O) group.