900800-02-4

Upstream product

• 626-02-8 3-Iodophenol 
• 93267-04-0 N-(tert-butoxycarbonyl)-L-3-iodoalanine methyl ester 
• 24424-99-5 di-tert-butyl dicarbonate 
• 587-33-7 m-tyrosine 
• 75677-04-2 3-<3-(benzyloxy)phenyl>propanal 
• 167935-97-9 methyl (S)-2-amino-3-(3-hydroxyphenyl)propanoate 
• 34260-70-3 methyl (2S)-2-amino-3-(3-hydroxyphenyl)propanoate hydrochloride 
• 447461-06-5 methyl (Z)-2-(tert-butoxycarbonyl)amino-3-[(3-benzyloxy)phenyl]acrylate 
• 121056-95-9 trimethyl 2-(tert-butoxycarbonylamino)phosphonoacetate 
• 1700-37-4 3-Benzyloxybenzaldehyde 
• 447461-03-2 (S)-N^α-tert-butoxycarbonyl-(m-benzyloxy)phenylalanine methyl ester 

Downstream Products

• 447461-07-6 (S)-N^α-tert-butoxycarbonyl-m-{[(trifluoromethyl)sulfonyl]oxy}phenylalanine methyl ester 
• 900800-03-5 (S)-3-(3-allyloxy-phenyl)-2-tert-butoxycarbonylamino-propionic acid methyl ester 
• 447461-03-2 (S)-N^α-tert-butoxycarbonyl-(m-benzyloxy)phenylalanine methyl ester 
• 1024615-65-3 methyl N-{[(1,1-dimethylethyl)oxy]carbonyl}-3-(phenyloxy)-L-phenylalaninate 
• 222556-20-9 (S)-3-(3-(benzyloxy)phenyl)-2-((S)-2-((tert-butoxycarbonyl)amino)-3-methylbutanamido)propanoic acid 
• 222556-14-1 (S)-1-[(S)-3-(3-Benzyloxy-phenyl)-2-((S)-2-tert-butoxycarbonylamino-3-methyl-butyrylamino)-propionyl]-hexahydro-pyridazine-3-carboxylic acid methyl ester 
• 184176-05-4 methyl (S)-2-((tert-butyloxycarbonyl)amino)-3-(3-methoxyphenyl)propanoate 
• 1300035-21-5 methyl (S)-3-(2-bromo-5-methoxyphenyl)2-((tert-butyloxycarbonyl)amino)propanoate 

Relevant academic research and scientific papers

AMINO-ACID ANILIDES AS SMALL MOLECULE MODULATORS OF IL-17

The present invention relates to a compound according to formula I (I) and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.

SMALL MOLECULE MODULATORS OF IL-17

The present invention relates to a compound according to formula I and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to, to said compounds for use in therapy, to pharmaceutical compositions comprising said

Enhanced copper-mediated 18F-fluorination of aryl boronic esters provides eight radiotracers for PET applications

[18F]FMTEB, [18F]FPEB, [18F]flumazenil, [18F]DAA1106, [18F]MFBG, [18F]FDOPA, [18F]FMT and [18F]FDA are prepared from the corresponding arylboronic esters and [18

Synthesis of the southern tripeptide (C1-N12) of sanglifehrins using asymmetric organocatalysis

The tripeptide southern region of the novel cyclophilin binding natural product macrolides, namely sanglifehrins, is synthesized involving asymmetric organocatalysis as chirality-inducing step. List's asymmetric α-amination was used in the synthesis of th

Evidence for the role of tetramethylethylenediamine in aqueous negishi cross-coupling: Synthesis of nonproteinogenic phenylalanine derivatives on water

The structure of the alkylzinc-tetramethylethylenediamine (TMEDA) cluster cation 3 has been determined in the gas phase by a combination of tandem mass spectrometry, infrared multiphoton dissociation (IRMPD) spectroscopy, and DFT calculations. Both sets of experimental results establish the existence of a strongly stabilizing interaction of TMEDA with the zinc cation. High-level DFT calculations on the alkylzinc-TMEDA cluster cation 3 allowed the identification of two low energy conformers, each featuring a four-coordinate zinc atom with a bidentate TMEDA ligand, and internal coordination from the carbonyl group of the Boc group to zinc. The experimental IRMPD spectrum is reproduced with an appropriately weighted combination of the IR spectra of the two conformers identified by theory. DFT calculations on the structure of the alkylzinc halide 2 with coordinated TMEDA using the PCM model of water solvent suggest that TMEDA can promote ionization of the zinc-iodine bond in organozinc iodides under aqueous conditions, providing a credible explanation for the role of TMEDA in stabilizing the carbon-zinc bond. Reaction of the serine-derived iodide 1 with aryl iodides "on water", promoted by nano zinc in the presence of PdCl2 (Amphos) 2 (5 mol %) and TMEDA, leads to the formation of protected phenylalanine derivatives 4 in reasonable yields. In the case of ortho-substituted aryl iodides and aryl iodides that are solids at room temperature, conducting the reaction at 65°C gives improved results. In all cases, the product 5 of reductive dimerization of the iodide 1 is also isolated.

Much improved conditions for the Negishi cross-coupling of iodoalanine derived zinc reagents with aryl halides

(Chemical Equation Presented) A combination of Pd2(dba) 3 and SPhos (1:2 molar ratio) is an excellent precatalyst for the Negishi cross-coupling of the serine-derived organozinc reagent 2 with aryl halides, including previously difficult ortho-substituted examples. In the case of meta- and para-substituted aryl halides, Pd-loadings of 0.5 mol % give satisfactory results. Use of 2-iodoaniline as substrate gives the lactam 12 in good yield. 2009 American Chemical Society.

Macrocyclic BACE-1 inhibitors acutely reduce Aβ in brain after po application

A series of macrocyclic peptidic BACE-1 inhibitors was designed. While potency on BACE-1 was rather high, the first set of compounds showed poor brain permeation and high efflux in the MDRI-MDCK assay. The replacement of the secondary benzylamino group wi

Thiol-based angiotensin-converting enzyme 2 inhibitors: P1′ modifications for the exploration of the S1′ subsite

Explorations of the S1′ subsite of ACE2 via modifications of the P1′ methylene biphenyl moiety of thiol-based metalloprotease inhibitors led to improvements in ACE2 selectivity versus ACE and NEP, while maintaining potent ACE2 inhibi

Macrocyclic Compounds Useful as Bace Inhibitors

The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS

The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.