776296-12-9

Upstream product

• 101861-59-0 3,5-dibromoquinoline 
• 124-41-4 sodium methylate 
• 6931-17-5 3-methoxyquinoline 
• 5332-24-1 3-bromoquinoline 

Downstream Products

• 877457-51-7 [3-(3-methoxy-quinolin-5-ylcarbamoyl)-cyclohexylmethyl]-carbamic acid tert-butyl ester 
• 881656-52-6 3-methoxy-quinoline-5-carbaldehyde 

Relevant academic research and scientific papers

Synthetic method of 3-methoxyquinoline-5-amine

The embodiment of the invention discloses a synthesis method of 3-methoxyquinoline-5-amine, relates to the technical field of synthesis of heterocyclic compounds, and aims to effectively synthesize the 3-methoxyquinoline-5-amine. The synthesis method comprises the following steps: taking 5-bromo-3-methoxyquinoline and benzophenone imine as raw materials, carrying out a coupling reaction at 45-120 DEG C to obtain an intermediate compound, and treating the intermediate compound at 25-30 DEG C by using hydroxylamine hydrochloride under an alkaline condition to obtain 3-methoxyquinoline-5 amine. The synthesis method provided by the embodiment of the invention is used for synthesizing the quinoline compound.

INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN

Disclosed are small molecule inhibitors of ανβ6 integrin, and methods of using them to treat a number of diseases and conditions. Applicants have discovered novel ανβ6 integrin inhibitor compounds and evaluated the possession, performance and utility of representative examples of such compounds, both for biochemical potency (e.g., using the assay of Example 7 to evaluate fluorescence polarization assays of compounds for ανβ6 binding) and in vitro permeability properties (e.g., using the assay of Example 8 to evaluate MDCK permeability).

Mapping the reactivity of the quinoline ring-system – Synthesis of the tetracyclic ring-system of isocryptolepine and regioisomers

Bromoquinolines (2-bromoquinoline – 8-bromoquinoline and 5-bromo-3-methoxyquinoline) and 2-aminophenylboronic acid hydrochloride were subjected to Suzuki-Miyaura cross-coupling conditions resulting in formation of the desired biaryl systems in good yields. The resulting biaryls were then subjected to palladium catalyzed C–H activation/C–N bond formation utilizing PdCl2(dppf). The reactions revealed large differences in reactivity depending on the attachment point for the 2-aminophenyl group on the quinoline. The variation in the reactivity was rationalized based on the electron distribution around the quinoline ring-system.

New quinolinic derivatives as melatonergic ligands: Synthesis and pharmacological evaluation

New series of melatonergic ligands issued from two methoxy-quinolinic scaffolds (2-MQ and 3-MQ), were designed and synthesized. Herein we report the synthetic scheme and pharmacological results of the new prepared compounds. Investigation of compound 11a, the strict 2-MQ analogue, revealed the promising potential of this series. Therefore, pharmacomodulation of the acetamide function of 11a has led to compounds with different pharmacological profiles and the emergence of an MT2selectivity. Besides, sulphonamide 11b showed the most important MT2selectivity of this series (167 folds) while methyl and ethyl-ureas 11f and 11g represented the most potent melatonergic ligands of this study.

Design, synthesis, and characterization of novel tetrahydropyran-based bacterial topoisomerase inhibitors with potent anti-gram-positive activity

There is an urgent need for new antibacterial drugs that are effective against infections caused by multidrug-resistant pathogens. Novel nonfluoroquinolone inhibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) have the potential

5-Quinoline derivatives having an anti-bacterial activity

The present invention describes novel anti-bacterial compounds of the formula (I). These compounds are, amongst others, of interest as inhibitors of DNA gyrase and topoisomerases, for example of topoisomerase II and IV.

CYCLOHEXYL OR PIPERIDINYL CARBOXAMIDE ANTIBIOTIC DERIVATIVES

The invention relates to antibiotic cyclohexyl or piperidinyl carboximide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl;one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRX, RX being a halogen atom;either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH═CH or CH2CH2;each of R3, R4, R5, R6, R7, and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9—COOH is naturally occurring amino acid or dimethylaminoglycine;and to salts of such compounds of formula (I).

New Piperidine Antibiotics

The invention relates to novel, antibacterially active piperidine derivatives of the formula wherein one of U and V represents N, the other represents N or CH; M represents CH2CH2, CH═CH, CH(OH)CH(OH), CH(OH)CH2, CH(NHsub

ETHANOL OR 1,2-ETHANEDIOL CYCLOHEXYL ANTIBIOTIC DERIVATIVES

The invention relates to antibiotic ethanol or 1,2-ethanediol cyclohexyl derivatives of formula (I) wherein R1 represents (C1-C4)alkoxy; one or two of U, V, W and X represent(s) N and the remaining represent each independently CH or, in the case of V or X

CYCLOHEXYL OR PIPERIDINYL CARBOXAMIDE ANTIBIOTIC DERIVATIVES

The invention relates to antibiotic cyclohexyl or piperidinyl carboxamide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl; one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRx, Rx being a halogen atom; either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH=CH or CH2CH2; each of R3, R4, R5, R6, R7 and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9-COOH is a naturally occurring amino acid or dimethylaminoglycine; and to salts of such compounds of formula (I).