321527-88-2

Upstream product

• 79-37-8 oxalyl dichloride 
• 66493-39-8 4-(N-tert-butoxycarbonyl)aminobenzoic acid 
• 150-13-0 4-amino-benzoic acid 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 1323993-27-6 3-{4-[5-(4-tert-butoxycarbonylamino-phenyl)-[1,3,4]oxadiazol-2-yl]-3-fluorophenyl}-2-[(5-p-tolyl-furan-2-carbonyl)-amino]-propionic acid 
• 1323992-39-7 5-[5-(4-tert-butoxycarbonylamino-phenyl)-[1,2,4]oxadiazol-3-yl]-2-[(5-p-tolyl-furan-2-carbonyl)-amino]-indan-2-carboxylic acid 

Relevant academic research and scientific papers

Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma

Interleukin 1 (IL-1) receptor-Associated kinases (IRAKs) are serine/threonine kinases that play critical roles in initiating the innate immune response against foreign pathogens. Additionally, dysregulation of IRAK1 signaling plays a role in neoplastic di

Exploring the ability of dihydropyrimidine-5-carboxamide and 5-benzyl-2,4-diaminopyrimidine-based analogues for the selective inhibition of L. major dihydrofolate reductase

To tackle leishmaniasis, search for efficient therapeutic drug targets should be pursued. Dihydrofolate reductase (DHFR) is considered as a key target for the treatment of leishmaniasis. In current study, we are interested in the design and synthesis of selective antifolates targeting DHFR from L. major. We focused on the development of new antifolates based on 3,4-dihydropyrimidine-2-one and 5-(3,5-dimethoxybenzyl)pyrimidine-2,4-diamine motif. Structure activity relationship (SAR) studies were performed on 4-phenyl ring of dihydropyrimidine (26–30) template. While for 5-(3,5-dimethoxybenzyl)pyrimidine-2,4-diamine, the impact of different amino acids (valine, tryptophan, phenylalanine, and glutamic acid) and two carbon linkers were explored (52–59). The synthesized compounds were assayed against LmDHFR. Compound 59 with the IC50 value of 0.10 μM appeared as potent inhibitors of L. major. Selectivity for parasite DHFR over human DHFR was also determined. Derivatives 55–59 demonstrated excellent selectivity for LmDHFR. Highest selectivity for LmDHFR was shown by compounds 56 (SI = 84.5) and 58 (SI = 87.5). Compounds Antileishmanial activity against L. major and L. donovani promastigotes was also performed. To explore the interaction pattern of the synthesized compounds with biological macromolecules, the docking studies were carried out against homology modelled LmDHFR and hDHFR targets.

ANTIBODY DRUG CONJUGATES OF KINESIN SPINDEL PROTEIN (KSP) INHIBITORS WITH ANTIB7H3-ANTIBODIES

The present application relates to novel binder drug conjugates (ADCs), to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for the treatment and/or prophylaxis of diseases and to the use of these ADCs for preparing medicaments for treatment and/or prophylaxis of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.

Thieme Chemistry Journals Awardees - Where Are They Now? Bis(2-pyridyl)amides as Readily Cleavable Amides under Catalytic, Neutral, and Room-Temperature Conditions

Mild solvolytic cleavage of bis(2-pyridyl)amide under neutral and room-temperature conditions is described. The inherently stable amide was readily activated by catalytic amounts of metal cations to react with alcohols. Based on X-ray crystallographic analysis, the primary driving force was considered to be amide distortion induced by the metal coordination of two pyridyl groups in a bidentate fashion without affecting the amide functionality. The compatibility of the acid/base-sensitive functionalities and the absence of racemization during solvolysis highlight the mildness of the present protocol.

Palladium-Catalyzed Carbon Isotope Exchange on Aliphatic and Benzoic Acid Chlorides

An operationally simple protocol for a palladium-catalyzed 13CO and 14CO exchange with activated aliphatic and benzoic carbonyls is presented. Several 13C and 14C building blocks, natural product derivatives, an

ANTIBODY DRUG CONJUGATES (ADCS) AND ANTIBODY PRODRUG CONJUGATES (APDCS) WITH ENZYMATICALLY CLEAVABLE GROUPS

The present invention relates to novel binder-prodrug conjugates (APDCs) where binders are conjugated with inactive precursor compounds of kinesin spindle protein inhibitors, and to antibody-drug conjugates ADCs and to processes for producing these APDCs and ADCs.

Heterogenization of chiral mono oxazoline ligands by grafting onto mesoporous silica MCM-41 and their application in copper-catalyzed asymmetric allylic oxidation of cyclic olefins

A series of chiral 4-oxazolinylaniline ligands 8 were conveniently synthesized on a gram scale from inexpensive and commercially available 4-aminobenzoic acid in four steps. The obtained organic chiral ligands have been covalently grafted onto ordered mesoporous silicas MCM-41 and the resulting inorganic–organic hybrid materials have been characterized by thermogravimetric analysis (TGA), differential thermal analysis (DTA), powder X-ray diffraction, BET and BJH nitrogen adsorption–desorption methods, energy-dispersive X-ray spectroscopy (EDX), CHN analysis, scanning electron microscopy (SEM), and Fourier transform infrared spectroscopy (FT-IR). The catalytic and induced asymmetric effects of the chiral copper (I) complexes of these new chiral supported heterogeneous catalysts on the asymmetric allylic oxidation of cycloolefins were investigated under different conditions. Reactions using the catalyst exhibited moderate to good enantioselectivities, up to 80%, and good yields, up to 95% better than the corresponding homogeneous reaction. The catalyst could be recovered easily and reused five times without remarkable loss of reactivity, yield, or enantioselectivity. This is, to the best of our knowledge, the first heterogenization of chiral 4-oxazolinylaniline ligands on an inorganic (silica) surface and their application as a heterogeneous catalyst in the asymmetric Kharash–Sosnovsky reaction.

Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors

Fibroblast growth factor receptors (FGFRs) are important targets for cancer therapy. Herein, we describe the design, synthesis, and biological evaluation of a novel series of 1H-pyrazolo[3,4-b]pyridine derivatives as potent and selective FGFR kinase inhibitors. On the basis of its excellent in vitro potency and favorable pharmacokinetic properties, compound 7n was selected for in vivo evaluation and showed significant antitumor activity in a FGFR1-driven H1581 xenograft model. These results indicated that 7n would be a promising candidate for further drug development.

CYSTOBACTAMIDES

The present invention provides cystobactamides of formula (I) and the use thereof for the treatment or prophylaxis of bacterial infections:

Acylative Suzuki coupling of amides: Acyl-nitrogen activation via synergy of independently modifiable activating groups

A highly efficient palladium-catalyzed acylative cross-coupling of carboxylic amides with arylboronic acids has been achieved via synergistic activation of the Cacyl-N bond by independently modifiable activating groups. Coupling of amides features not only good functional group tolerance but also modifiable reactivities to overcome steric hindrance. This journal is