213136-30-2

Upstream product

• 501-53-1 benzyl chloroformate 
• 26531-82-8 (S)-methyl 2-amino-2-(4-hydroxyphenyl)acetate 
• 57591-61-4 methyl (R)-2-amino-2-(4-hydroxyphenyl)acetate hydrochloride 
• 22818-40-2 D-4-hydroxyphenylglycine 
• 32462-30-9 (S)-hydroxyphenylglycine 
• 67-56-1 methanol 
• 26787-75-7 (R)-2-(((benzyloxy)carbonyl)amino)-2-(4-hydroxyphenyl)acetic acid 
• 37763-23-8 D-2-p-hydroxyphenylglycine methyl ester 

Downstream Products

• 600738-17-8 N-benzyloxycarbonyl-4-tert-butoxy-R-phenylglycine methyl ester 
• 199392-93-3 Benzyl (R)-2-hydroxy-1-(4-methoxyphenyl)ethylcarbamate 
• 100929-33-7 (R)-2-amino-2-(4-methoxyphenyl)-1-ethanol 

Relevant academic research and scientific papers

Intermediate of RORgamma inhibitor and preparation method thereof

The invention belongs to the technical field of drugs, in particular to an intermediate of a RORgamma inhibitor and a preparation method thereof. The intermediate is as shown in a formula (I). The method has the advantages of being easily available in raw material, concise in process, economic and environment-friendly, high in yield and the like. The formula is as shown in the description.

D - P-hydroxy-glycine derivatives and their preparation method and application

The invention discloses a D-hydroxy phenylglycine derivative. Please see the formula of the D-hydroxy phenylglycine derivative in the specification. D-hydroxy phenylglycine serves as a parent body, amino groups and carboxyl groups of the D-hydroxy phenylglycine are reasonably modified, a phenolic hydroxyl group is connected with an aromatic nucleus type hydrophobic group through a connector, the D-hydroxy phenylglycine derivative which is novel in structure is constructed, compounds capable of promoting the secreting activity of GLP-1 and/or inhibiting the activity of Nav1.7 are screened out, the preparation method of the compounds is simple and can be used for preparing GLP-1secernent and/or Nav1.7 inhibitors, and the D-hydroxy phenylglycine derivative has potential application prospects in the fields of diabetes treatment drugs and/or neuropathy pain treatment drugs. Please see the formula in the specification.

Electronic effects of aryl-substituted bis(oxazoline) ligands on the outcome of asymmetric copper-catalysed C-H insertion and aromatic addition reactions

The effect of the modification of bis(oxazoline) ligands on the outcome of copper-catalysed C-H insertion and aromatic addition reactions is described. In general, these reactions display minimum sensitivity in terms of enantiocontrol to variation of the electronic properties of the aryl moiety of the ligand however, some influence is observed for C-H insertions employing naphthyl-substituted bis(oxazolines) and for aromatic addition reactions of biphenyl diazo ketone substrates. The synthesis of the modified bis(oxazolines), which include four novel structures, is also described.

Syntheses of amino alcohols and chiral C2-symmetric bisoxazolines derived from O-alkylated R-4-hydroxyphenylglycine and S-tyrosine

Chiral C2-symmetric bisoxazolines 1b-f and 2b,c, derived from 4′-O-alkylated R-4-hydroxyphenylglycine or S-tyrosine, were prepared. As intermediates, a series of chiral amino alcohols possessing substituted phenolic groups was prepared and fully characterized.

Synthesis of Isodityrosine, Dityrosine and Related Compounds by Phenolic Oxidation of Tyrosine and Phenylglycine Derivatives Using an Electrochemical Method

The phenolic oxidation of L-tyrosine derivatives by electrolysis and zinc reduction produced the coupling products leading to isodityrosine and dityrosine.The oxidation mode could be controlled by altering halogen substituents (Br or I) at two ortho positions of phenol groups.Additionally, this methodology was applied to 4-hydroxy-D-phenylglycine derivatives, providing the correspoinding oxidative products.