1455028-46-2

Upstream product

• 243665-10-3 (E)-3-(4-fluorophenyl)-N-methoxy-N-methylacrylamide 
• 459-32-5 (E)-4-fluorocinnamic acid 
• 459-32-5 4-fluorocinnamic acid 
• 1355061-76-5 C₁₁H₁₂FNO₂ 
• 1774-47-6 trimethylsulfoxonium iodide 
• 42153-74-2 (+)-(S_S)-S-methyl-S-phenyl-N-(p-tolylsulphonyl)sulphoximine 

Downstream Products

• 1455028-47-3 (1S,2S)-1-(2-(4-fluorophenyl)cyclopropyl)ethanone 

Relevant academic research and scientific papers

Stereoselective Synthesis of (Sulfonimidoyl)cyclopropanes with (R)-PhSO(NTs)CH2Cl and α,β-Unsaturated Weinreb Amides: Tuning the of Selectivity between C-Cl and C-S Bond Cleavage

(Sulfonimidoyl)cyclopropanes have become the subject of special interest since they combine the advantages of two chemical leads (cyclopropane and sulfoximine). However, their synthesis is limited, and the stereoselective synthesis of optically enriched (sulfonimidoyl)cyclopropanes still remains an unsolved task. Here we report the first stereoselective (sulfonimidoyl)cyclopropanation reaction using α,β-unsaturated Weinreb amides and (R)-PhSO(NTs)CH2Cl [(R)-1]. This reaction possesses a broad substrate scope, and the products can be easily transformed into other useful cyclopropyl-containing and/or sulfonimidoyl-containing compounds. The Weinreb amide group and the counter cation of the base were found to be important for the selective C-Cl bond cleavage. The first (sulfonimidoyl)cyclopropanation of α,β-unsaturated carbonyl compounds with (R)-PhSO(NTs)CH2Cl was achieved to afford optically enriched (sulfonimidoyl)cyclopropanes in good yields with excellent diastereoselectivities. The reaction shows a broad substrate scope. The Weinreb amide group and the counter cation of the base were found to be important for the selective C-Cl bond cleavage.

Discovery and optimization of Lu AF58801, a novel, selective and brain penetrant positive allosteric modulator of alpha-7 nicotinic acetylcholine receptors: Attenuation of subchronic phencyclidine (PCP)-induced cognitive deficits in rats following oral administration

In this Letter, we describe a chemical lead optimization campaign starting from a novel, weak α7 nicotinic acetylcholine receptor positive allosteric modulator (PAM) hit from a HTS screen. Exploration of the structure-activity relationships for α7 PAM potency, intrinsic hepatic clearance, the structure-property relationships for lipophilicity, and thermodynamic solubility, led to the identification of Lu AF58801: a potent, orally available, brain penetrant PAM of the α7 nicotinic acetylcholine receptor, showing efficacy in a novel object recognition task in rats treated subchronically with phencyclidine (PCP).

Positive Allosteric Modulators of MGLUR2

The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the centr