41863-52-9

Upstream product

• 91103-47-8 N-(tert-butoxycarbonyl)-D-alanine methyl ester 
• 24424-99-5 di-tert-butyl dicarbonate 
• 57400-52-9 1-Butoxycarbonyl-L-alanin-N'-4-picolyloxycarbonylhydrazid 
• 113707-01-0 Boc-Ala-OCet 
• 15761-38-3 L-N-Boc-Ala 
• 530-62-1 1,1'-carbonyldiimidazole 
• 28875-17-4 (S)-N-(tert-butoxycarbonyl)alanine methyl ester 
• 7803-57-8 hydrazine hydrate 
• 119706-04-6 BOC-Ala-OBg 
• 144800-33-9 Boc-Ala-OAbc 
• 51814-53-0 N-tert-butoxycarbonyl-L-alanine ethyl ester 

Downstream Products

• 716329-44-1 (R)-tert-butyl (1-(1,3,4-oxadiazol-2-yl)ethyl)carbamate 
• 1202635-25-3 C₂₈H₃₀F₃N₇O₄ 
• 1332700-42-1 tert-butyl N-[(S)-1-methyl-2-oxo-2-(2-cyclohexylidenehydrazino)ethyl]carbamate 
• 1332700-48-7 diethyl (S)-[1-(2-{2-[(tert-butoxycarbonyl)amino]propanoyl}hydrazino)cyclohexyl]phosphonate 
• 1357304-18-7 C₂₁H₃₄N₄O₇S 
• 1357304-19-8 N-(Boc)-alaninyl-azasulfurylglycinyl-D-phenylalanine tert-butyl ester 
• 1357304-07-4 C₂₁H₃₄N₄O₇S 

Relevant academic research and scientific papers

Synthesis of 5 H -Pyrrolo[3,4- b ]pyrazine-Based Peptidomimetics

A range of 5H-pyrrolo[3,4-b]pyrazine-based peptidomimetics were designed, and their efficient synthesis starting from 5-imino-5H-pyrrolo[3,4-b]pyrazin-7-amine by subsequent interaction with N-protected amino acid hydrazides and amino acid esters with N,N-carbonyldiimidazole as the coupling agent was elaborated.

Unveiling the active isomer of cycloalanopine, a cyclic opine from: Lactobacillus rhamnosus LS8, through synthesis and analog production

Opines are widely distributed natural products formed by the reductive condensation of amino acids with α-keto acids or carbonyls of carbohydrates. They have important biological roles in bacteria, higher plants, fungi, invertebrates and mammals, including humans. An unusual cyclic opine of undefined stereochemistry, cycloalanopine, was previously isolated from Lactobacillus rhamnosus LS8 and reported to have antimicrobial activity against both Gram-negative and Gram-positive bacteria. In this work, we report a three-step strategy to synthetically access pure isomers of this cyclic compound and analogs thereof. In the key step, acyclic bis-hydrazides can be oxidized with (diacetoxyiodo) benzene to corresponding cyclic N,N-diacylhydrazides. The three cycloalanopine isomers, along with several analogs, were synthesized and tested against a panel of Gram-positive and Gram-negative bacteria. We identified the active isomer as the meso compound: (4R,6S)-4,6-dimethyl-1,2,5-triazepan-3,7-dione. Additionally, a glycine derivative, (R)-4-methyl-1,2,5-triazepan-3,7-dione, was ascertained to be more potent. This compound was active against both Gram-positive and Gram-negative organisms with the strongest potency against Escherichia coli and Acinetobacter baumannii, an opportunistic pathogen found in hospital-derived infections.

Amino Acid Functionalized Organotin Trichlorides and Their Tin Sulfide Clusters

We present a new synthesis of functionalized tin sulfide clusters via organotin trichlorides with boc-protected amino acids (RAAcSnCl3). In this work we used non-polar (alanine, valine, leucine, phenylalanine and methionine), polar/neutral (serine and tyrosine) and basic (histidine) amino acids. We obtained single crystals from a Boc-protected valine derivative of the originally used organotin trichloride R1SnCl3 [R1 = CMe2CH2C(O)Me] and determined its structure by means of X-ray diffraction. A subsequent reaction with sulfide sources led to a variety of respective cluster structures. By using either (Me3Si)2S or Na2S, the reaction product turns out to be the defect-heterocubane cluster [(RAAcSn)3S4Cl] or the “doppeldecker”-type cluster [(RAAcSn)4S6], respectively, according to 119Sn NMR spectroscopy.

2,4,5-TRISUBSTITUTED 1,2,4-TRIAZOLONES USEFUL AS INHIBITORS OF DHODH

The present invention provides triazolone compounds compounds of general formula (I) : in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

1,3-THIAZOL-2-YL SUBSTITUTED BENZAMIDES

The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.

New tetrahydropyrido pyrimidinecarboxylic compound or salt thereof

To provide a compound having an inhibitory activity for an androgen receptor. A tetrahydropyridopyrimidine compound represented by the following general formula (I) or a pharmaceutically acceptable thereof (in the formula, X and R are as defined in the specification).

NOVEL PYRROLIDINE DERIVED BETA 3 ADRENERGIC RECEPTOR AGONISTS

The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.

P2X3 AND/OR P2X2/3 COMPOUNDS AND METHODS

The present application provides novel compounds and methods for preparing and using these compounds. In one embodiment, the compounds are of the structure of formula (I), wherein R1-R4 are defined herein. In a further embodiment, these compounds are useful in method for regulating one or both of the P2X3 or P2X2/3 receptors. In another embodiment, these compounds are useful for treating pain in patients by administering one or more of the compounds to a patient.

3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH

The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are described herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant I DH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH

The invention is directed to a formula (I), or a pharmamceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.