177472-60-5

Upstream product

• 1421676-97-2 ethyl (1R,2R)-2-((di-tert-butoxycarbonyl)amino)cyclopropanecarboxylate 
• 613261-19-1 (±)-cis-ethyl 2-((tert-butoxycarbonyl)amino)cyclopropanecarboxylate 
• 613261-19-1 trans-ethyl 2-(tert-butoxycarbonylamino)-1-cyclopropane carboxylate 

Downstream Products

• 177472-48-9 (+)-(1S,2R)-cis-<2-(tert.-butoxycarbonylamino)-cyclopropyl>-methanol 
• 162129-49-9 ((1R,2S)-2-Hydroxymethyl-cyclopropyl)-carbamic acid tert-butyl ester 
• 561055-28-5 tert-Butyl ((1R,2R)-2-((benzyloxy)methyl)cyclopropyl)carbamate 

Relevant academic research and scientific papers

Indoleamine-2,3-dioxygenase inhibitor as well as preparation method and application thereof

The invention provides a compound as shown in a formula (I). The invention also relates to a pharmaceutical composition containing the compound of the formula (I) and application of the compound to preparation of an indoleamine-2,3-dioxygenase (IDO) inhibitor drug. The compound prepared by the method of the invention has an obvious inhibiting effect on IDO protease and is stable in metabolism in vivo. The compound or a pharmaceutical composition thereof provided by the invention can be used for preparing the IDO inhibitor drug, and can also be used for preparing medicines for preventing and/ortreating diseases with pathological characteristics of an IDO-mediated tryptophan metabolic pathway.

Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations

Exploration of small selective ligands for the nicotinic acetylcholine receptors (nAChRs) based on acetylcholine (ACh) has led to the development of potent agonists with clear preference for the α4β2 nAChR, the most prevalent nAChR subtype in the central nervous system. In this work we present the continuation of these efforts aimed at increasing this subtype selectivity by introduction of conformational restriction in the carbamoylcholine homologue, 3-(dimethylaminobutyl) dimethylcarbamate (DMABC). Our results highlight the importance of the N-carbamoyl substitution in α4β2-subtype selectivity. Moreover, we have confirmed the non-linear conformation of DMABC bound to nAChRs suggested by recent crystal structures of the compound in complex with the Lymnaea stagnalis ACh binding protein.

Highly enantioselective synthesis of cyclopropylamine derivatives via Ru(II)-pheox-catalyzed direct asymmetric cyclopropanation of vinylcarbamates

The Ru(II)-Pheox-catalyzed asymmetric cyclopropanation of vinylcarbamates with diazoesters resulted in the corresponding cyclopropylamine derivatives in high yield and excellent diastereoselectivity (up to 96:4) and enantioselectivity (up to 99% ee).

Enantiomerically pure cyclopropanoid nucleoside analogues: Synthesis and analysis

Enantiomerically pure cyclopropanoid nucleoside analogues were synthesized by a chemo-enzymatic approach starting from racemic dialkyl 1,2-cyclopropane dicarboxylates. Their enantiomeric purity can be easily verified by HPLC analysis using Chiralcel OD or Chiralcel OD-R columns.

Synthesis of racemic carbocyclic cyclopropanoid nucleoside analogues

As further representatives of a novel class of carbocyclic nucleoside analogues (±)-cis- and (±)-trans-(2-hydroxymethylcyclopropyl)-uracil, -thymine, and -inosine were synthesized from the corresponding dialkyl 1,2-cyclopropane dicarboxylates.

Synthesis of Cyclopropyl Carbocyclic Nucleosides

As representatives of a novel class of carboxylic nucleoside analogues (+/-)-cis-, (-)-cis and (+/-)-trans 9-(2-hydroxymethylcyclopropyl)-adenine (= -methanol) were synthesized from the corresponding dialkyl 1,2-cyclopropane dicarboxylates.