329025-40-3

Upstream product

• 175221-03-1 (1S,2S)-cyclopropane-1,2-dicarboxylic acid mono-(1R,2S,5R)-(5-isopropyl-2-methyl-cyclohexyl) ester 
• 96149-00-7 (1S,2S)-cyclopropane-1,2-dicarboxylic acid bis-(1R,2S,5R)-(5-isopropyl-2-methyl-cyclohexyl) ester 
• 34212-59-4 bis(1R,2S,5R)-5-methyl-2-(propan-2-yl)cyclohexyl butanedioate 

Downstream Products

• 329025-42-5 (2S,1'S,2'S)-N-[(R)-α-phenylglycinol]-[2'-carbomenthyloxycyclopropyl]-glycinonitrile 
• 117857-93-9 (2S,1'S,2'S)-α-(2-carboxycyclopropyl)glycine 
• 329025-41-4 2-carbomenthyloxy (1S,2S)-cyclopropane-1-carboxaldehyde 

Relevant academic research and scientific papers

RADIOLABELED CANNABINOID RECEPTOR 2 LIGAND

The present invention relates to a compound of formula (I) wherein R1, R2, and R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a radiolabeled ligand.

Identification and Preclinical Development of a 2,5,6-Trisubstituted Fluorinated Pyridine Derivative as a Radioligand for the Positron Emission Tomography Imaging of Cannabinoid Type 2 Receptors

Despite the broad implications of the cannabinoid type 2 receptor (CB2) in neuroinflammatory processes, a suitable CB2-targeted probe is currently lacking in clinical routine. In this work, we synthesized 15 fluorinated pyridine derivatives and tested their binding affinities toward CB2 and CB1. With a sub-nanomolar affinity (Ki for CB2) of 0.8 nM and a remarkable selectivity factor of >12,000 over CB1, RoSMA-18-d6 exhibited outstanding in vitro performance characteristics and was radiofluorinated with an average radiochemical yield of 10.6 ± 3.8% (n = 16) and molar activities ranging from 52 to 65 GBq/μmol (radiochemical purity > 99%). [18F]RoSMA-18-d6 showed exceptional CB2 attributes as demonstrated by in vitro autoradiography, ex vivo biodistribution, and positron emission tomography (PET). Further, [18F]RoSMA-18-d6 was used to detect CB2 upregulation on postmortem human ALS spinal cord tissues. Overall, these results suggest that [18F]RoSMA-18-d6 is a promising CB2 PET radioligand for clinical translation.

PYRIDINE AND PYRAZINE DERIVATIVES AS PREFERENTIAL CANNABINOID 2 AGONISTS

The invention relates to a compound of formula (I), wherein A1, A2 and R1-R5 are as defined in the description and in the claims. The compound of formula (I) can be used as cannabinoid 2 preferential agonist.

Four Stereoisomers of 2-Aminomethyl-1-cyclopropanecarboxylic Acid: Synthesis and biological evaluation

Here, we report a practical method for asymmetric synthesis of cyclopropane-fused GABA analogs. Starting from 2-furaldehyde, the cis-isomer (CAMP) was synthesized over 10 steps; (1)- and (+)-CAMP￠HCl were synthesized by employing d- and l-menth

An efficient and stereoselective synthesis of (2S,1′S,2′S)-2-(carboxycyclopropyl) glycine (LCCG-I): Conformationally constrained L-glutamate analogues

Conformationally restricted metabotropic glutamate receptor agonist (2S,1′S,2′S)-2-(Carboxycyclopropyl) glycine (LCCG-I) 1 have been efficiently synthesized in a stereoselective manner. A convenient five step synthesis of 1 from readily available (-)-dime