86778-91-8

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 23239-35-2 (S)-2-amino-2-methyl-3-phenylpropanoic acid 
• 103-79-7 1-phenyl-acetone 
• 64384-47-0 2-amino-3-phenyl-2-methylpropanenitrile 
• 1132-26-9 2-methyl-3-phenylalanine 
• 1443008-10-3 (S)-2-amino-N-((1S,2S)-2-hydroxy-1,2-diphenylethyl)-N,2-dimethyl-3-phenylpropanamide 
• 100-39-0 benzyl bromide 
• 171898-25-2 5-benzyl-N-(tert-butoxycarbonyl)-2-(tert-butyldimethylsiloxy)pyrrole 
• 171898-22-9 (+/-)-5-benzyl-1-(tert-butoxycarbonyl)-2,5-dihydropyrrol-2-one 
• 853304-11-7 tert-butyl 1-hydroxy-2-methyl-3-phenylpropan-2-ylcarbamate 
• 100-44-7 benzyl chloride 
• 1393737-29-5 (S)-4-benzyl-3-tert-butoxycarbonyl-4-methyl-2-oxazolidinone 
• 1393737-59-1 (S)-4-benzyl-4-methyl-2-oxazolidinone 
• 1393737-50-2 (S)-(4-benzyl-2-oxazolidinon-4-yl)methyl p-toluenesulfonate 

Downstream Products

• 74814-07-6 Tyr-D-Ala-Gly-Phe(αMe) 
• 74814-06-5 Tyr-D-Ala-Gly-Phe(αMe)-Leu 
• 129713-59-3 N-tert-butoxycarbonyl-L-α-methylphenylalanyl-L-cysteinyl(Acm)-D-tryptophyl-L-leucine methyl ester 
• 74825-82-4 tert-butoxycarbonyl-α-methyl-L-phenylalanyl-L-valine benzyl ester 
• 192064-93-0 (S)-2-((S)-2-tert-Butoxycarbonylamino-2-methyl-3-phenyl-propionylamino)-3-(1H-imidazol-4-yl)-propionic acid methyl ester 
• 1428736-37-1 (2S)-2-[(tert-butoxycarbonyl)amino]-2-methyl-3-phenylpropanamide 
• 1428736-40-6 (2R,5S)-5-benzyl-5-methyl-2-(pyridine-2-yl)imidazolidine-4-one 
• 1428736-42-8 (2S,5S)-5-benzyl-5-methyl-2-(pyridine-2-yl)imidazolidine-4-one 
• 1428736-44-0 (2R,5S)-5-benzyl-2,5-dimethyl-2-(pyridine-2-yl)imidazolidine-4-one 
• 1428736-46-2 (2S,5S)-5-Benzyl-2,5-dimethyl-2-(pyridine-2-yl)imidazolidine-4-one 
• 1132-26-9 2-methyl-3-phenylalanine 
• 88084-32-6 N-(phenylacetyl)-L-prolyl-DL-α-methylphenylalanyl-L-arginine 
• 88084-36-0 N-(3-phenylpropanoyl)-L-prolyl-DL-α-methylphenylalanyl-L-arginine 
• 88084-37-1 N-(5-phenylpentanoyl)-L-prolyl-DL-α-methylphenylalanyl-L-arginine 

Relevant academic research and scientific papers

METHOD FOR SYNTHESIZING OPTICALLY ACTIVE a-AMINO ACID USING CHIRAL METAL COMPLEX COMPRISING AXIALLY CHIRAL N-(2-ACYLARYL)-2-[5,7-DIHYDRO-6H-DIBENZO[c,e]AZEPIN-6-YL] ACETAMIDE COMPOUND AND AMINO ACID

Objects of the present invention are to provide an industrially applicable method for producing an optically active α-amino acid in high yield and in a highly enantioselective manner, to provide a simple production method of an optically active α,α-disubstituted α-amino acid, and to provide an intermediate useful for the above production methods of an optically active α-amino acid and an optically active α,α-disubstituted α-amino acid. The present invention provides a production method of an optically active α-amino acid or a salt thereof, the production method comprising introducing a substituent into the α carbon in the α-amino acid moiety of a metal complex represented by the following Formula (1): by an alkylation reaction, an aldol reaction, the Michael reaction, or the Mannich reaction, and releasing an optically pure α-amino acid enantiomer or a salt thereof by acid decomposition of the metal complex.

METHOD FOR SYNTHESIZING OPTICALLY ACTIVE α-AMINO ACID USING CHIRAL METAL COMPLEX COMPRISING AXIALLY CHIRAL N-(2-ACYLARYL)-2-[5,7-DIHYDRO-6H-DIBENZO[c,e]AZEPIN-6-YL]ACETAMIDE COMPOUND AND AMINO ACID

Objects of the present invention are to provide an industrially applicable method for producing an optically active ±-amino acid in high yield and in a highly enantioselective manner, to provide a simple production method of an optically active ±,±-disubstituted ±-amino acid, and to provide an intermediate useful for the above production methods of an optically active ±-amino acid and an optically active ±,±-disubstituted ±-amino acid. The present invention provides a production method of an optically active ±-amino acid or a salt thereof, the production method comprising introducing a substituent into the ± carbon in the ±-amino acid moiety of a metal complex represented by the following Formula (1): by an alkylation reaction, an aldol reaction, the Michael reaction, or the Mannich reaction, and releasing an optically pure ±-amino acid enantiomer or a salt thereof by acid decomposition of the metal complex.

Enantiocatalytic activity of substituted 5-benzyl-2-(pyridine-2-yl) imidazolidine-4-one ligands

Currently, asymmetric synthesis represents one of the main streams of organic synthesis. Although an extensive research has been carried out in this area, the synthesis of chiral compounds with the required enantiomeric purity is still a challenging issue. Herein, we focus on the preparation of new enantioselective catalysts based on pyridine-imidazolidinones. The substituted 5-benzyl-2-(pyridine-2-yl)imidazolidine-4-ones 5-8 were prepared by condensation of chiral amino acid amides (α-methylDOPA and α- methylphenylalanine) with 2-acetylpyridine and pyridine-2-carbaldehyde. The individual isomers of the described ligands 5-8 were separated chromatographically. The copper(II) complexes of these chiral ligands were studied as enantioselective catalysts for the asymmetric Henry reaction of substituted aldehydes with nitromethane or nitroethane. The ligands containing a methyl group at the 2-position of the imidazolidinone ring 6a and 8a exhibit a high degree of enantioselectivity (up to 91% ee). The nitroaldols derived from nitroethane (2-nitropropan-1-ols) were obtained with a comparable enantiomeric purity to derivatives of 2-nitroethanol. This group of ligands represents a new and promising class of enantioselective catalysts, which deserve further attention.

Synthesis of quaternary α-methyl α-amino acids by asymmetric alkylation of pseudoephenamine alaninamide pivaldimine

The utility of pseudoephenamine as a chiral auxiliary for the alkylative construction of quaternary α-methyl α-amino acids is demonstrated. The method is notable for the high diastereoselectivities of the alkylation reactions, for its versatility with respect to electrophilic substrate partners, and for its mild hydrolysis conditions, which provide α-amino acids without salt contaminants. Alternatively, α-amino esters can be obtained by direct alcoholysis.

Non-enzymatic diastereoselective asymmetric desymmetrization of 2-benzylserinols giving optically active 4-benzyl-4-hydroxymethyl-2- oxazolidinones: Asymmetric syntheses of α-(hydroxymethyl)phenylalanine, N-Boc-α-methylphenylalanine, cericlamine and BIRT-377

A reaction of (S)-2-benzyl-2-(α-methylbenzyl)amino-1,3-propanediol (S)-4a and 2-chloroethyl chloroformate, and the subsequent addition of DBU gave (4R,αS)-4-benzyl-4-hydroxymethyl-3-(α-methylbenzyl)-2-oxazolidinone (4R)-5a (92% de) via a diastereoselective asymmetric desymmetrization process. Debenzylation of (4R)-5a using trifluoromethanesulfonic acid and anisole in MeNO2 gave (R)-4-benzyl-4-hydroxymethyl-2-oxazolidinone (R)-15a, which was converted into (R)-(α-hydroxymethyl)phenylalanine (7) in two steps. N-Boc-α-methylphenylalanine (8), cericlami0ne (9) and BIRT-377 (10) were also synthesized using these asymmetric desymmetrization and debenzylation.

Piperazine Compounds Having Herbicidal Action

The present invention relates to piperazine compounds of the general formula I defined below and to their use as herbicides. Moreover, the invention relates to compositions for crop protection and to a method for controlling unwanted vegetation. R1 is selected from the group consisting of halogen, cyano, nitro, Z—C(=O)—R12, phenyl and a 5- or 6-membered heterocyclic radical which has 1, 2, 3 or 4 heteroatoms selected from the group consisting of O, N and S as ring atoms, where phenyl and the heterocyclic radical are unsubstituted or may have 1, 2, 3 or 4 substituents R1a; Z is a covalent bond or a CH2 group; R12 is hydrogen, C1-C6-alkyl, C3-C6-cycloalkyl, C2-C6-alkenyl, C5-C6-cycloalkenyl, C2-C6-alkynyl and the like; R2 is hydrogen, halogen, nitro, cyano, C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C1-C4-alkoxy, C1-C4-haloalkoxy, benzyl or a group S(O)nR21 in which R21 is C1-C4-alkyl or C1-C4-haloalkyl and n is 0, 1 or 2; R3 is hydrogen or halogen; R4 is C1-C4-alkyl, C3-C4-alkenyl or C3-C4-alkynyl; R5 is hydrogen, C1-C4-alkyl, C3-C4-alkenyl, C3-C4-alkynyl or a group C(=O)R51 in which R51 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy; R6 is C1-C4-alkyl, C1-C4-hydroxyalkyl or C1-C4-haloalkyl; R7, R8 independently of one another are hydrogen, OH, C1-C4-alkoxy, C1-C4-haloalkyloxy, C1-C4-alkyl or C1-C4-haloalkyl; R9, R10 independently of one another are selected from the group consisting of hydrogen, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C1-C4-alkoxy and C1-C4-haloalkoxy; and R11 is hydrogen or C1-C4-alkyl; and the agriculturally useful salts of these compounds.

Herbicidally Active Composition

The present invention relates to herbicidally active compositions comprising at least one piperazinedione compound of the formula I in which: Rx, Ry are each hydrogen or together are a chemical bond; R1 is cyano or nitro; R2 is hydrogen, fluorine, chlorine, C1-C2-alkyl, ethenyl or C1-C2-alkoxy; R3 is fluorine or hydrogen; R4 is methyl; R5 is hydrogen, methyl or ethyl; R6 is hydrogen, methyl or ethyl; and R7 is hydrogen or halogen; and at least one further active compound selected from the group consisting of b1) lipid biosynthesis inhibitors; b2) acetolactate synthase inhibitors (ALS inhibitors); b3) photosynthesis inhibitors; b4) protoporphyrinogen-IX oxidase inhibitors, b5) bleacher herbicides; b6) enolpyruvyl shikimate 3-phosphate synthase inhibitors (EPSP inhibitors); b7) glutamine synthetase inhibitors; b8) 7,8-dihydropteroate synthase inhibitors (DHP inhibitors); b9) mitose inhibitors; b10) inhibitors of the synthesis of very long chain fatty acids (VLCFA inhibitors); b11) cellulose biosynthesis inhibitors; b12) decoupler herbicides; b13) auxin herbicides; b14) auxin transport inhibitors; b15) other herbicides, and C) safeners.

Tricyclic Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease

The present invention is directed to tricyclic compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also

Amino-substituted heterocycles, compositions thereof, and methods of treatment therewith

Provided herein are Heterocyclic Compounds having the following structure: wherein R1, R2, X, Y and Z are as defined herein, compositions comprising an effective amount of a Heterocyclic Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heterocyclic Compound to a patient in need thereof.

TRICYCLIC BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE

The present invention is directed to tricyclic compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also