121006-14-2

Upstream product

• 6335-80-4 ethyl 3-(benzylamino)butanoate 
• 21759-74-0 ethyl (Z)-3-(benzylamino)-2-butenoate 
• 1020-67-3 ethyl 3-(benzylamino)crotonate 
• 507444-65-7 methyl 3-(benzylamino)butanoate 

Downstream Products

• 98014-59-6 Benzyl-(3-hydroxy-1-methyl-propyl)-carbamic acid tert-butyl ester 
• 1384850-07-0 N,N-dibenzyl-3-bromobutan-1-amine 
• 7730-40-7 1-benzyl-2-methylazetidine 
• 823785-71-3 (+/-)-3-benzyl-4-methyl-[1,2,3]oxathiazinane-2,2-dioxide 
• 1413930-80-9 (E)-ethyl 2-(1-benzyl-5-methylpyrrolidin-2-ylidene)acetate 

Relevant academic research and scientific papers

Synthesis of 1-alkyl-2-(trifluoromethyl)azetidines and their regiospecific ring opening toward diverse α-(trifluoromethyl)amines via intermediate azetidinium salts

A convenient approach toward nonactivated 1-alkyl-2-(trifluoromethyl) azetidines as a new class of constrained azaheterocycles was developed starting from ethyl 4,4,4-trifluoroacetoacetate via imination, hydride reduction, chlorination, and base-induced ring closure. Furthermore, the reactivity profile of these 2-CF3-azetidines was assessed by means of quaternization and subsequent regiospecific ring opening at C4 of the azetidinium intermediates by oxygen, nitrogen, carbon, sulfur, and halogen nucleophiles, pointing to a clear difference in reactivity compared to azetidines bearing other types of electron-withdrawing groups at C2.

3-[1,4]OXAZEPANE-4-PYRIMIDONE DERIVATIVES

A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom, C-F or the like; R1 represents a C1-C3 alkyl group; Y represents oxygen atom or N-R7; R2, R3, R4, R5, R6 and R7 each independently represents hydrogen atom, a C1-C6 alkyl group, or a group represented by the formula (II): which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

Chemo- and diastereoselective reduction of β-enamino esters: A convenient synthesis of both cis- and trans-γ-amino alcohols and β-amino esters

Convenient procedures for the chemo- and diastereoselective reduction of b-enamino esters 1 are described. Both cis- and trans-γ-amino alcohols 2 or b-amino esters 3 can be prepared by reduction of b-enamino esters 1, readily available starting materials, with the use of inexpensive reagents Na/i-PrOH or NaHB(OAc)3/AcOH, respectively, and the appropriate reduction conditions. The mechanisms and diastereoselectivities for the reductions are discussed. The relative configurations and conformations of the diastereoisomeric γ-amino alcohols 2 and β-amino esters 3 obtained are established by 1H and 13C NMR study and unequivocally set by their cyclic derivatives tetrahydro-1,3-oxazines 4.

Stereocontrolled Synthesis of Cis-Fused Hydroisoquinolines by an Intramolecular Diels-Alder Reaction of (Z)-Dienes

An efficient stereocontrolled synthesis highly functionalized cis-fused octahydroisoquinolines via an intramolecular Diels-Alder reaction of (Z)-dienes is described.