22428-85-9

Upstream product

• 29648-66-6 4-methylenecyclohexanone 
• 51656-90-7 8-methylene-1,4-dioxaspiro[4.5]decane 
• 4746-97-8 cyclohexanedione monoethylene ketal 
• 13482-22-9 4-hydroxycyclohexanone 
• 2065-66-9 methyl-triphenylphosphonium iodide 

Downstream Products

• 106434-94-0 1-Methoxy-4-methylencyclohexan 
• 1272667-39-6 ((1S,4S)-4-(5-(3-(7-oxabicyclo[2.2.1]heptan-1-ylmethoxy)phenyl)-4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexyl)methanol 
• 1272667-38-5 (1S,4S)-4-(5-(3-(7-oxabicyclo[2.2.1]heptan-1-ylmethoxy)phenyl)-4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanecarbaldehyde 
• 1272667-53-4 ((1S,4S)-4-(5-(3-(7-oxabicyclo[2.2.1]heptan-1-ylmethoxy)phenyl)-4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexyl)methyl methanesulfonate 
• 1272667-52-3 5-(3-(7-oxabicyclo[2.2.1]heptan-1-ylmethoxy)phenyl)-7-((1s,4s)-4-(azidomethyl)cyclohexyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine 
• 1272666-89-3 2-(3-((7-oxabicyclo[2.2.1]heptan-1-yl)methoxy)phenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane 
• 1272670-06-0 5-(3-(7-oxabtcyclo[2.2.1]heptan-1-ylmethoxy)phenyl)-7-((1S,4S)-4-(aminomethyl)cyclohexyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine 
• 1398924-07-6 d9-1-[4-fluoro-3-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenoxymethyl]-7-oxa-bicyclo[2.2.1]heptane 
• 1398924-03-2 1-[4-fluoro-3-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenoxymethyl]-7-oxa-bicyclo[2.2.1]heptane 
• 1398924-05-4 1-(3-bromo-4-fluoro-phenoxymethyl)-7-oxa-bicyclo[2.2.1]heptane 
• 1398923-91-5 1-[2-fluoro-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenoxymethyl]-7-oxa-bicyclo[2.2.1]heptane 
• 1398923-73-3 1-[2-fluoro-3-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenoxymethyl]-7-oxa-bicyclo[2.2.1]heptane 
• 1398923-75-5 1-(3-bromo-2-fluoro-phenoxymethyl)-7-oxa-bicyclo[2.2.1]heptane 
• 29648-66-6 4-methylenecyclohexanone 

Relevant academic research and scientific papers

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors

Taking the pyrrolopyrimidine derived IGF-1R inhibitor NVP-AEW541 as the starting point, the benzyl ether back-pocket binding moiety was replaced with a series of 2-cyclic ether methyl ethers leading to the identification of novel achiral [2.2.1]-bicyclic ether methyl ether containing analogues with improved IGF-1R activities and kinase selectivities. Further exploration of the series, including a fluorine scan of the 5-phenyl substituent, and optimisation of the sugar-pocket binding moiety identified compound 33 containing (S)-2-tetrahydrofuran methyl ether 6-fluorophenyl ether back-pocket, and cis-N-Ac-Pip sugar-pocket binding groups. Compound 33 showed improved selectivity and pharmacokinetics compared to NVP-AEW541, and produced comparable in vivo efficacy to linsitinib in inhibiting the growth of an IGF-1R dependent tumour xenograft model in the mouse.

FLUOROPHENYL BICYCLIC HETEROARYL COMPOUNDS

The present invention provides a compound of formula (I); a method for manufacturing the compounds of the invention, and its use as a IGF-1R inhibitor. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

HYDROXY SUBSTITUTED ISOQUINOLINONE DERIVATIVES

The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.

ETHER DERIVATIVES OF BICYCLIC HETEROARYLS

The invention relates to compounds of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; such compounds as a medicament; such compounds for the treatment of a proliferative disease

Aminothiazole substituted penicillins and antibacterial compositions thereof

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or in-vivo hydrolysable ester thereof: STR1 wherein R1 is hydrogen or an amino protecting group and R is substituted methyl; optionally substituted C2-12 alkyl, alkenyl or alkynyl; carbocyclyl; aryl or heterocyclyl. These compounds have antibacterial properties, and therefore are of use in the treatment of bacterial infections in humans and animals caused by a wide range of organisms.

Chemo-Selectivity of Group-VIII Metal Catalysts in Hydrogenation of Nonconjugated Enones

The chemo-selectivity of group-VIII metal catalysts has been examined in the hydrogenation of nonconjugated enones at ambient temperature under an atmospheric pressure of hydrogen.A cobalt catalyst gave high yields of unsaturated alcohols from trialkylated olefinic ketones.Osmium showed the highest selectivity among platinum metal catalysts for the reduction of the carbonyl bond in the hydrogenation of trialkylated olefinic ketones.The hydrogenation of mono- and dialkylated olefinic ketone ordinarily proceeded with a preferential saturation of the olefinic function, regardless of the catalysts.The hydrogenation of 4-methylene- and 4-ethylidenecyclohexanone was accompanied by the formation of diethyl acetals over ruthenium, rhodium, and palladium black catalysts in an ethanol solvent.The acetals were not detected in the hydrogenation of the other enones and over the other catalysts.In addition, the chemoselectivity on the hydrogenation of acyclic enones was examined over nickel and cobalt catalysts treated with small amounts of alkali and carbon monoxide.The amount of unsaturated alcohols increased when the catalyst was treated with alkali in the case of di- and trialkylated olefinic ketones, whereas the characteristics of cobalt, which selectively reduces the ketonic function in trialkylated olefinic ketoones, were completely missing when cobalt was treated with carbon monoxide.

Deamination Reactions, 46. - Decomposition of 1-Alkenylcyclopropanediazonium Ions

1-(2-Propenyl)- (10a), 1-(2-methyl-2-propenyl)- (10b), and 1-(3-butenyl)cyclopropanediazonium ions (35) have been generated by alkaline cleavage of the analogous nitrosocarbamates in methanol.Their major reaction paths are cyclopropyl-allyl tranformation (67 - 81percent), elimination to give alkylidenecyclopropanes (13 - 21percent), nucleophilic displacement (4 - 6percent), and 1,2-H shift (1 - 5percent).Participation of the double bond with formation of spirocyclic products was found to be small (0.5 - 1.2percent) with 10a, b and negligible with 35.The 2-methylene-5-hexenyl cations (39) arising from 35 underwent cyclization (intramolecular electrophilic addition, 39 --> 42) in competition with nucleophilic capture, but did not undergo a degenerate Cope rearrangement (39 39').