50778-40-0

Upstream product

• 89-94-1 trans-6-methyl-3-cyclohexene-1-carboxaldehyde 
• 583-60-8 2-Methylcyclohexanone 
• 97575-40-1 cis-2-Methyl-1-<4-brom-benzolsulfonyloxymethyl>-cyclohexan, cis-2-Methylcyclohexanemethyl Brosylate 
• 7605-54-1 methyl (1S*,2R*)-2-methylcyclohexanecarboxylate 
• 7076-91-7 (+-)-cis-2-methyl-cyclohexanecarboxylic acid 
• 3937-45-9 cis-1-hydroxymethyl-2-methylcyclohexane 
• 591-49-1 1-methylcyclohex-1-ene 
• 201230-82-2 carbon monoxide 
• 39163-61-6 (+/-)-trans-2-methyl-cyclohexene-⁽⁴⁾-carbaldehyde-⁽¹⁾-semicarbazone 
• 13149-22-9 1-Aethoxymethyl-2-methyl-cyclohexanol-⁽¹⁾ 
• 421-20-5 Methyl fluorosulfonate 
• 66730-34-5 2-(cyclohex-1-en-1-yl)benzo[d]thiazole 
• 917-54-4 methyllithium 
• 90951-24-9 (+/-)-trans-2-methyl-cyclohexanecarbaldehyde-semicarbazone 

Downstream Products

• 101654-53-9 1-bromo-2-methyl-cyclohexanecarbaldehyde 
• 1533-89-7 trans-1-methyl-2-vinylcyclohexane 
• 1533-89-7 cis-1-methyl-2-vinylcyclohexane 
• 3937-46-0 (+/-)-(trans-2-Methyl-cyclohexyl)-methanol 

Relevant academic research and scientific papers

Absence of the alleged retardation of the Diels-Alder reaction for dienes bearing a neighbouring hydroxy substituent

Contrary to earlier observations the diene 1 reacts readily in Diels-Alder additions. With N-methylmaleimide the stereoisomeric adducts 10a and 10b are formed in equal quantities. With maleic anhydride, ring-opening accompanies adduction to give 11 and two stereoisomers of gross structure 12. Dienes 1,9 (X = OMe) and 9 (X = H) react at similar rates with N-methylmaleimide, discounting the alleged intramolecular retardation due to through space interaction between the hydroxy group and the diene system.

Fragment-Based Discovery of Pyrazolopyridones as JAK1 Inhibitors with Excellent Subtype Selectivity

Herein, we report the discovery of a series of JAK1-selective kinase inhibitors with high potency and excellent JAK family subtype selectivity. A fragment screening hit 1 with a pyrazolopyridone core and a JAK1 bias was selected as the starting point for our fragment-based lead generation efforts. A two-stage strategy was chosen with the dual aims of improving potency and JAK1 selectivity: Optimization of the lipophilic ribose pocket-targeting substituent was followed by the introduction of a variety of P-loop-targeting functional groups. Combining the best moieties from both stages of the optimization afforded compound 40, which showed excellent potency and selectivity. Metabolism studies in vitro and in vivo together with an in vitro safety evaluation suggest that 40 may be a viable lead compound for the development of highly subtype-selective JAK1 inhibitors.

Ligand-Controlled Direct Hydroformylation of Trisubstituted Olefins

The direct hydroformylation of trisubstituted olefins has been achieved with a combination of a Rh(I) catalyst and a π-acceptor phosphorus (briphos) ligand. A sterically bulky briphos ligand with a large cone angle that forms a 1:1 complex with Rh(I) is found to be reactive for the hydroformylation of trisubstituted olefins. The aldehyde products were obtained with high diastereoselectivity (>99:1) and regioselectivity (49%-81%).