2843-16-5

Upstream product

• 3240-34-4 [bis(acetoxy)iodo]benzene 
• 108-24-7 acetic anhydride 
• 1184-88-9 sodium pivalate 
• 75-98-9 Trimethylacetic acid 
• 117756-41-9 (3-hydroxy-2,2-dimethyl-propyl)acetate 
• 126-30-7 2,2-Dimethyl-1,3-propanediol 
• 4835-90-9 3-Hydroxy-2,2-dimethylpropanoic acid 
• 81778-04-3 3-acetoxy-2,2-dimethyl-propionic acid methyl ester 
• 7440-44-0 pyrographite 
• 18516-19-3 2,2-dimethyl-3-oxopropyl 4-methylbenzenesulfonate 
• 64-19-7 acetic acid 
• 2843-19-8 3-amino-2,2-dimethylpropanoic acid, hydrochloride salt 
• 75-36-5 acetyl chloride 
• 16184-79-5 3-acetoxy-2,2-dimethyl-1-propanal 

Downstream Products

• 58908-51-3 β-(Acetoxy)peroxypivalinsaeure-tert.-butylester 
• 1439618-36-6 3-(benzyloxy(2-chlorobenzyl)amino)-2,2-dimethyl-3-oxopropyl acetate 
• 1439618-45-7 N-(benzyloxy)-N-(2-chlorobenzyl)-3-hydroxy-2,2-dimethylpropanamide 
• 4835-90-9 3-Hydroxy-2,2-dimethylpropanoic acid 
• 1354043-56-3 C₂₂H₂₂FN₇O₃ 
• 1376603-54-1 C₂₄H₂₄FN₇O₄ 
• 1236364-22-9 C₂₉H₂₉Cl₃N₂O₄ 
• 937724-28-2 C₃₅H₄₅N₃O₃ 
• 937724-27-1 C₃₆H₄₄N₄O₃ 
• 937724-26-0 C₃₆H₄₇N₃O₄ 
• 937724-25-9 C₃₆H₄₇N₃O₄ 
• 937724-24-8 C₃₅H₄₄FN₃O₃ 

Relevant academic research and scientific papers

CONDENSED BI-HETEROCYCLES AS INHIBITING AGENTS FOR BRUTON'S TYROSINE KINASE

Provided are compounds of Formula (I): Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, A1, B1, B2, Q1 and Q2 are as defined herein; and methods for their use and production.

Cobalt-Catalyzed Deprotection of Allyl Carboxylic Esters Induced by Hydrogen Atom Transfer

A brief, efficient method has been developed for the removal of the allyl protecting group from allyl carboxylic esters using a Co(II)/TBHP/(Me2SiH)2O catalytic system. This facile strategy displays excellent chemoselectivity, functional group tolerance, and high yields. This transformation probably occurs through the hydrogen atom transfer process, and a Co(III)-six-membered cyclic intermediate is recommended.

Direct β-C(sp3)-H Acetoxylation of Aliphatic Carboxylic Acids

The controlled construction of defined oxidation patterns is one of the key aspects in the synthesis of natural products and bioactive molecules. Towards this goal, we herein report a novel protocol for the Pd-catalyzed direct β-C(sp3)-H acetoxylation of aliphatic carboxylic acids. The protocol enables the use of free carboxylic acids in one step and without the need of introducing specialized strong directing groups. In our studies, we found that the use of a "traceless base" was crucial for the development of a synthetically useful transformation. Furthermore, the synthetic utility of the products obtained was demonstrated by their use in subsequent transformations.

AMINOPYRIDINE DERIVATIVES AS PHOSPHATIDYLINOSITOL PHOSPHATE KINASE INHIBITORS

The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula: (I) where A, B, R1, X1, X2, and W are described herein.

Gold(I)/copper(II)-cocatalyzed tandem cyclization/semipinacol reaction: Construction of 6-Aza/Oxa-Spiro[4.5]decane skeletons and formal synthesis of (±)-halichlorine

A simple and efficient strategy for the construction of 6-aza/oxa-spiro[4.5]decane skeletons under the cocatalysis of gold(I)/copper(II) was developed, and its potential utility was demonstrated by a formal synthesis of the biologically active marine alkaloid (±)-halichlorine.

3,4-DISUBSTITUTED 1 H-PYRAZOLE AND 4,5-DISUBSTITUTED THIAZOLE INHIBITORS OF SYK

The present invention relates to the use of novel compounds of formula (I), wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.

Nickel-catalyzed site-selective amidation of unactivated C(sp 3)-H bonds

Intramolecular dehydrogenative cyclization of aliphatic amides was achieved on unactivated sp3 carbon atoms by a nickel-catalyzed C-H bond functionalization process with the assistance of a bidentate directing group. The reaction favors the C-H bonds of β-methyl groups over the γ-methyl or β-methylene groups. Additionally, a predominant preference for the β-methyl C-H bonds over the aromatic sp2 C-H bonds was observed. Moreover, this process also allows for the effective functionalization of benzylic secondary sp3 C-H bonds. β-Lactams from nickel catalysis: Intramolecular dehydrogenative cyclization of aliphatic amides was achieved on unactivated sp3 carbon atoms by a nickel-catalyzed C-H bond functionalization process with the assistance of a bidentate directing group (see scheme).

Antimicrobial N-(2-chlorobenzyl)-substituted hydroxamate is an inhibitor of 1-deoxy-d-xylulose 5-phosphate synthase

N-(2-Chlorobenzyl)-substituted hydroxamate, readily produced by hydrolysis of ketoclomazone, was identified as an inhibitor of 1-deoxy-d-xylulose 5-phosphate synthase (DXS), with an IC50 value of 1.0 μM. The compound inhibited the growth of Haemophilus influenzae. A convenient spectroscopic method for assaying DXS using NADPH-lactate dehydrogenase (LDH) is also reported.

ETHYNYL DERIVATIVES

The present invention relates to ethynyl derivatives of formula (I) wherein X is N or C-R1; Y is N or C-R2; Z is CH or N; R4 is a 6-membered aromatic substituent containing 0, 1 or 2 nitrogen atoms, optionally substituted by 1 to 3 groups, selected from halogen, lower alkyl, lower alkoxy or NRR'; R1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, lower hydroxyalkyl, lower cycloalkyl or is heterocycloalkyl optionally substituted with hydroxy or alkoxy; R2 is hydrogen, CN, lower alkyl or heterocycloalkyl; R and R' are independently from each other hydrogen or lower alkyl; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula (I) are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.

ETHYNYL COMPOUNDS USEFUL FOR TREATMENT OF CNS DISORDERS

The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.