123795-38-0

Upstream product

• 57292-44-1 N-Boc-D-(4-Cl)Phe-OH 
• 74-88-4 methyl iodide 
• 637-87-6 1-Chloro-4-iodobenzene 
• 76757-90-9 N-(tert-butoxycarbonyl)-D-tyrosine methyl ester 
• 1254365-35-9 (Z)-methyl 2-((tert-butoxycarbonyl)amino)-3-(4-chlorophenyl)acrylate 
• 139377-26-7 (4R,5S,2R)-4-chloro-1-<2-azido-3-oxo-3-(2-oxo-4-methyl-5-phenyl-3-oxazolidinyl)propyl>benzene 
• 139377-25-6 (4R,5S)-4-chloro-1-<3-oxo-3-(2-oxo-4-methyl-5-phenyl-3-oxazolidinyl)propyl>benzene 
• 139377-27-8 (R)-2-Azido-3-(4-chloro-phenyl)-propionic acid 
• 1027659-22-8 C₁₄H₁₇ClO₃ 
• 2019-34-3 3-(4-chlorophenyl)propanoic acid 
• 24424-99-5 di-tert-butyl dicarbonate 
• 134166-72-6 D-p-chlorophenylalanine methyl ester 
• 139377-28-9 D-(-)-N-diaza-4-chlorophenylalanine methyl ester 

Downstream Products

• 57292-44-1 N-Boc-D-(4-Cl)Phe-OH 
• 276861-14-4 (R)-N-(2-chloroacetyl)-4-chlorophenylalanine methyl ester 
• 1610691-87-6 (R)-N-[N-(2,2-dimethoxyethyl)glycinyl]-4-chlorophenylalanine methyl ester 
• 149818-98-4 methyl (R)-α-<<(1,1-dimethylethoxy)carbonyl>amino><1,1'-biphenyl>-4-propanoate 
• 398147-95-0 (4R)-(N'-methyl-N'-tert-butyl-oxycarbonyl-amino)-4-(4-chlorobenzyl)-but-2-enoic acid 
• 203932-47-2 [2-(4-chloro-phenyl)-1-formyl-ethyl]-methyl-carbamic acid tert-butyl ester 
• 203932-48-3 2-(tert-butoxycarbonyl-methyl-amino)-3-(4-chloro-phenyl)-propionic acid methyl ester 
• 139377-47-2 D-(-)-N-<(1,1-dimethylethoxy)carbonyl>-4-<3-<1-acetyl>amino>-2-oxo-2-ethoxyethyl>phenoxy>phenylalanine methyl ester 

Relevant academic research and scientific papers

Preparation method of sacubitril intermediate

The invention relates to the technical field of synthesis of medical intermediates, in particular to a preparation method of a sacubitril intermediate, which comprises the following steps: 1) reacting a raw material compound III with phosphorus trihalide to obtain a compound II; and 2) reacting the compound II with phenylhydrazine in the presence of a catalyst and an additive to obtain a sacubitril intermediate, namely a compound I. According to the invention, cheap phosphorus trihalide is selected to replace expensive and highly toxic trifluoromethanesulfonic anhydride, and cheap phenylhydrazine and a catalyst palladium chloride are adopted. The method has the advantages of simple reaction operation, low cost and high yield, and is easier for industrial production of the compound I.

A Practical Method for Continuous Production of sp3-Rich Compounds from (Hetero)Aryl Halides and Redox-Active Esters

A practically useful coupling reaction between aromatic halides and redox-active esters was realized by nickel catalysis through the use of a packed zinc bed column in continuous flow. Multiple reuse of the column showed a negligible decrease in efficiency, affording high space/time yields. A wide range of substrates, including a number of heteroaryl halides and polyfunctional materials were coupled in generally good yields. Longer-time and larger-scale experiments further demonstrates the robustness of the system.

A diastereoselective construction of pyrazinoisoquinoline skeletons via tandem cyclization of phenylalanine derivatives: A facile synthesis of optically active pyrazinoisoquinolines

A facile and stereocontrolled construction of optically active pyrazinoisoquinoline skeletons based on tandem cyclization of enantiopure phenylalanine derivatives was examined. The reaction provided optically active 6,11b-trans pyrazinoisoquinoline ring systems in excellent diastereoselectivity, and this method was applicable to the cyclization of phenylalanine derivatives with diverse substituents.

Discovery of pyrrolopyrimidine inhibitors of Akt

The discovery and optimization of a series of pyrrolopyrimidine based protein kinase B (Pkb/Akt) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent inhibition of all three Akt isoforms and knockdown of phospho-PRAS40 levels in LNCaP cells and tumor xenografts.

N-[(R,R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-ylcarbamoyl)-allyl]-N- methyl-3,5-bis-trifluoromethyl-benzamide: An orally active neurokinin NK1/NK2 antagonist

The stereoselective synthesis of N-[(R,R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-ylcarbamoyl)-allyl]-N-methyl-3 ,5-bis-trifluoromethyl-benzamide (4) and its NK1 and NK2 receptor binding properties are reported. In addition the potent inhibitory effects in vivo on sar9-SP- and β-Ala-NKA-induced airway bronchoconstriction in guinea pigs are demonstrated. (C) 2000 Elsevier Science Ltd. All rights reserved.