88099-68-7

Upstream product

• 88099-67-6 methyl (2S)-2-(dibenzylamino)-3-hydroxypropanoate 
• 943437-44-3 methyl 2-(dibenzylamino)-3-hydroxypropanoate 
• 100-39-0 benzyl bromide 
• 911404-06-3 C₁₉H₂₃NO₅S 
• 100-44-7 benzyl chloride 
• 93527-55-0 (S)-2-(dibenzylamino)-3-hydroxypropanoic acid 

Downstream Products

• 1193100-06-9 C₁₇H₁₈FNO₂*ClH 
• 1609546-34-0 (R)-N,N-dibenzyl-2-fluoro-3-methoxypropan-1-amine 
• 1609545-83-6 (R)-4-(dibenzylamino)-3-fluoro-2-methylbutan-2-ol 
• 344413-78-1 (2R)-3-(dibenzylamino)-2-fluoropropan-1-ol 

Relevant academic research and scientific papers

NEW MACROCYCLIC LRRK2 KINASE INHIBITORS

Compounds of formula (I): wherein R, X1, X2, X3, Z1, Z2, Z3, A and Ra are as defined in the description. Medicaments.

HETEROARYL SUBSTITUTED NICOTINAMIDE COMPOUNDS

Disclosed are compounds of Formula (I) or salts thereof, wherein: HET is a heteroaryl selected from pyrazolyl, indolyl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-d]pyrimidinyl, pyrazolo[3,4-b]pyridinyl, pyrazolo[3,4-d]pyrimidinyl, 2,3-dihydro-1H-pyrrolo[2,3-b]pyridinyl, imidazo[4,5-b]pyridinyl, and purinyl, wherein said heteroaryl is substituted with Ra and Rb; and R1 and R2 are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.

PROCESS FOR PRODUCING -FLUORO- -AMINO ACIDS

By reacting a β-hydroxy-α-amino acid with sulfuryl fluoride (SO2F2) in the presence of an organic base, it is possible to produce an α-fluoro-β-amino acid of the formula [2]. By using a C8-12 tertiary amine having two or more alkyl g

Synthesis and pharmacological evaluation of novel γ-aminobutyric acid type B (GABAB) receptor agonists as gastroesophageal reflux inhibitors

We have previously demonstrated that the prototypical GABAB receptor agonist baclofen inhibits transient lower esophageal sphincter relaxations (TLESRs), the most important mechanism for gastroesophageal reflux. Thus, GABAB agonists could be exploited for the treatment of gastroesophageal reflux disease. However, baclofen, which is used as an antispastic agent, and other previously known GABAB agonists can produce CNS side effects such as sedation, dizziness, nausea, and vomiting at higher doses. We now report the discovery of atypical GABAB agonists devoid of classical GABAB agonist related CNS side effects at therapeutic doses and the optimization of this type of compound for inhibition of TLESRs, which has resulted in a candidate drug (R)-7 (AZD3355) that is presently being evaluated in man.

PROCESS FOR THE SYNTHESIS OF ALKYL PHOSPHINIC ACIDS BY INITIATION OF AN AMINE AND AN AMINEOXIDE

The present invention relates toa new process for the synthesis of alkyl phosphinic acids, and more particularly to a coupling reaction between an alkylhalide and a hypophosphorous acid derivative in the presence of an amine and an amineoxide.

PROCESS FOR THE SYNTHESIS OF ALKYL PHOSPHINIC ACIDS BY INITIATION OF AN AMINE AND AN AMINEOXIDE

The present invention relates to a new process for the synthesis of alkyl phosphinic acids, and more particularly to a coupling reaction between an alkylhalide and a hypophosphorous acid derivative in the presence of an amine and an amineoxide.

NEW PROCESS FOR THE PREPARATION OF PHOSPHINIC ACID

A new process for the synthesis of a compound of formula [Chemical formula should be inserted here. Please see paper copy] wherein A represents O or N; R?1? represents a C?1#191-C?6#191 alkyl; R?2? and R?3? each independently represents C?1#191-C?10#191 a

Stereochemistry of Catabolism of the DNA Base Thymine and of the Anticancer Drug 5-Fluorouracil

(2S)-3-Amino-2-methylpropanoic acid (6) and (2RS,3S)--3-amino-2-methylpropanoic acid (14) have been synthesized and used to provide an assay which shows that the catabolism of the DNA base thymine (1; R = Me) proceeds by overall anti addition of hydrogen to the pyrimidine at the si face at C-5 and the si face at C-6.X-Ray structure analysis of a derivative of the product of reaction of N,N-dibenzyl-L-serine methyl ester (15; R = Me) with (diethylamino)sulphur trifluoride followed by deprotection has shown it to be (2R)-3-amino-2-fluoropropanoic acid (19; R = H).This was identical with the product of catabolism of the anti-cancer drug 5-fluorouracil (1; R = F).Esters of (2R,3S)-- and (2R,3R)--3-amino-2-fluoropropanoic acids have been synthesized and used to provide an assay which shows that catabolism of the anti-cancer drug 5-fluorouracil (1; R = F) proceeds with the same absolute stereochemistry as is found in catabolism of thymine (1; R = Me).

Stereochemistry of the Metabolism of the DNA Base Thymine and the Drug 5-Fluorouracil

The enzyme dihydrothymine dehydrogenase reduces both the DNA base thymine and the anti-cancer drug 5-fluorouracil by overall trans addition of hydrogen, at the si-face at C-5 and the si-face at C-6.