79751-10-3

Upstream product

• 100945-15-1 N-(benzyloxycarbonyl)phosphonoglycine trimethyl ester 
• 100-52-7 benzaldehyde 
• 207396-31-4 (2S,3R)-N-benzyloxycarbonyl-3-phenylserine methyl ester 
• 1191124-96-5 N-benzyloxycarbonyl-α-(diphenylphosphono)glycine methyl ester 
• 621-84-1 O-benzyl carbamate 
• 79002-45-2 N-benzyloxycarbonyl-glycine 
• 127357-37-3 methyl 2-(benzyloxycarbonylamino)-2-methoxyacetate 

Relevant academic research and scientific papers

Silver-Promoted Direct Phosphorylation of Bulky C(sp2)-H Bond to Build Fully Substituted β-Phosphonodehydroamino Acids

A general and practical cross-dehydrogenative coupling protocol between readily available trisubstituted α,β-dehydro α-amino carboxylic esters and H-phosphites is described. This C(sp2)-H phosphorylation reaction proceeds with absolute Z-selectivity promoted by silver salt in a radical relay manner. The bulky tetrasubstituted β-phosphonodehydroamino acids were obtained in grams and added new modules to the toolkit for peptide modifications.

Stereoselective Synthesis of (E)-α,β-dehydroamino acid esters

Dehydroamino acid (Dhaa) is recognized as a useful tool or substrate for amino acid and peptide research. Although the stereoselective synthesis of the thermodynamically more stable Z-Dhaa has been well examined and established, the stereoselective synthesis of E-Dhaa has still remained to be a challenging synthetic task. In this paper, a stereoselective synthesis of E-Dhaa esters using a new (α-diphenylphosphono)glycine is described. The characteristic aspects of the new method are summarized as follows: (i) metal additives play an important role in the promotion of E-stereoselectivities. (ii) the use of NaI was effected for the synthesis of E-Dhaas bearing an aryl substituent and an amino functionality, (iii) MgBr2·OEt2 and ZnCl 2 contributed to improve the E-stereoselective synthesis of E-Dhaas bearing an alkyl substituent and an oxygen functionality, (iv) various protecting and functional groups were compatible under the reaction conditions, and (v) N-Cbz, Boc, and acyl-α-(diphenylphosphono)glycines were served for the stereoselective olefination reaction to provide the corresponding E-Dhaas. A variety of (E)-dehydroamino acid esters were stereoselectively synthesized by using (diphenylphosphono)glycinate. The stereoselectivity was influenced by metal additives. Various (E)-dehydroamino acid esters were prepared by the condensation reaction of the new phosphonates with easily available aldehydes by choosing the appropriate reaction conditions.

Efficient total synthesis of (-)-kaitocephalin

A highly dlastereoselectlve total synthesis of (-)-kaltocephalln, a novel antagonist of lonotroplc glutamate receptors, was accomplished In 12 steps starting from 5-substltuted proline ester via the aldol reaction with OBO-serlne aldehyde, (E)-selectlve α,β-dehydroamlno acid synthesis using a new HWE reagent, and catalytic hydrogenation.

CHEMICAL COMPOUNDS

The invention provides a new method for treating disorders associated with activation of the Notch signal transduction pathway comprising administering an effective amount of a compound of Formula (I), in free form or in a pharmaceutically acceptable salt

Regioselective synthesis of substituted pyrroles: Efficient palladium-catalyzed cyclization of internal alkynes and 2-amino-3-iodoacrylate derivatives

(Diagram presented) The first efficient and regioselective palladium-catalyzed cyclization of internal alkynes and 2-amino-3-iodoacrylates to give moderate to excellent yields of highly functionalized pyrroles has been developed. This approach is applicab

NOVEL LACTAMS AND USES THEREOF

Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid ? protein production and neurological disorders such as Alzheimer's disease.. These compounds inhibit γ secretase and thereby inhibit the production of amyloid ? protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.

Stereoselective syntheses of (E)-α,β-dehydroamino acids and (E)-α,β-dehydropeptides by stereospecific dehydration with 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC)

Highly stereoselective syntheses of (E)-α,β-dehydroamino acids and (E)-α,β-dehydropeptides have been achieved in good yields by stereospecific dehydration of threo-β-hydroxy-α-amino acid derivatives using 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC

Diastereoselective formation of (Z)-didehydroamino acid esters

The rearrangement of (E)-didehydroamino acid derivatives to the corresponding Z-derivatives under acid or basic catalysis as well as under the influence of radicals has been investigated. The condensation of N-benzyloxycarbonyl or N-tert-butoxycarbonyl protected alkyl 2-amino-2-(dimethoxyphosphoryl)acetates with aldehydes or ketones in dichloromethane in the presence of 1,8-diazabicyclo[5.4.0]undec-7-ene furnishes (Z)-didehydroamino acid ester derivatives diastereoselectively in excellent yields and with high purity.