443955-89-3

Usage

Uses

Used in Pharmaceutical Industry:
(2,3-Dihydro-[1,4]dioxino[2,3-c]pyridin-7-yl)methanol is used as a pharmaceutical intermediate for the synthesis of various medications. Its role in the development of new drugs is crucial, as it can contribute to the creation of innovative treatments for a range of medical conditions.
Used in Medicinal Chemistry Research:
In the field of medicinal chemistry, (2,3-Dihydro-[1,4]dioxino[2,3-c]pyridin-7-yl)methanol is used for studying its biological activity and potential applications in the treatment of certain medical conditions. This research aims to better understand the compound's properties and how it can be utilized to develop effective therapies.

Upstream product

• 59281-14-0 5-benzyloxy-2-hydroxymethyl-1H-pyridin-4-one 
• 443955-90-6 2,3-dihydro-[1,4]dioxino[2,3-c]pyridine-7-carbaldehyde 
• 736088-02-1 6-hydroxymethyl-3,4-pyridinediol 
• 106-93-4 ethylene dibromide 
• 31883-16-6 6-hydroxymethyl-3-hydroxy-4-pyridinone 
• 615568-25-7 2,3-dihydro-[1,4]dioxino[2,3-c]pyridine-7-carboxylic acid ethyl ester 
• 1314933-98-6 C₆H₉NO₃ 
• 1159266-59-7 5-(2-chloroethoxy)-2-(hydroxymethyl)-4H-pyran-4-one 
• 501-30-4 5-hydroxy-2-(hydroxymethyl)-4H-pyran-4-one 
• 15771-06-9 5-benzyloxy-2-hydroxymethyl-4H-pyran-4-one 
• 103893-45-4 5?hydroxy?2?tetrahydropyranyloxymethyl?4H?pyran?4?one 

Downstream Products

• 917836-01-2 (2,3-dihydro-[1,4]dioxino[2,3-c]pyridin-7-yl)methanamine 
• 1073632-76-4 1,1-dimethylethyl (2,3-dihydro[1,4]dioxino[2,3-c]pyridin-7-ylmethyl){6-[(diphenylmethylidene)amino]-1,2,3,4-tetrahydro-2-naphthalenyl}carbamate 
• 1073631-82-9 (R)-4-{6-[(2,3-dihydro[1,4]dioxino[2,3-c]pyridin-7-ylmethyl)amino]-5,6,7,8-tetrahydro-2-naphthalenyl}-6-(methyloxy)pyrido[2,3-b]pyrazin-3(4H)-one benzoate 
• 1073631-79-4 (S)-4-{6-[(2,3-dihydro[1,4]dioxino[2,3-c]pyridin-7-ylmethyl)amino]-5,6,7,8-tetrahydro-2-naphthalenyl}-6-(methyloxy)pyrido[2,3-b]pyrazin-3(4H)-one benzoate 
• 527681-13-6 2,3-dihydro-[1,4]dioxino[2,3-c]pyridine-7-carboxylic acid 
• 443955-90-6 2,3-dihydro-[1,4]dioxino[2,3-c]pyridine-7-carbaldehyde 

Relevant academic research and scientific papers

JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate

The discovery of a novel 2-aminotetrahydropyridine class of BACE1 inhibitors is described. Their pKa and lipophilicity were modulated by a pending sulfonyl group, while good permeability and brain penetration were achieved via intramolecular hydrogen bonding. BACE1 selectivity over BACE2 was achieved in the S3 pocket by a novel bicyclic ring system. An optimization addressing reactive metabolite formation, cardiovascular safety, and CNS toxicity is described, leading to the clinical candidate JNJ-67569762 (12), which gave robust dose-dependent BACE1-mediated amyloid β lowering without showing BACE2-dependent hair depigmentation in preclinical models. We show that 12 has a favorable projected human dose and PK and hence presented us with an opportunity to test a highly selective BACE1 inhibitor in humans. However, 12 was found to have a QT effect upon repeat dosing in dogs and its development was halted in favor of other selective leads, which will be reported in the future.

Development of the Convergent, Kilogram-Scale Synthesis of an Antibacterial Clinical Candidate Using Enantioselective Hydrogenation

Early chemical development studies into the best way of assembling AZD9742, an antibacterial drug candidate, have involved swapping the order of two reductive aminations. The orthogonally functionalized aminopiperidine partner for these couplings is now enantioselectively synthesized using ruthenium-catalyzed asymmetric hydrogenation. The challenge of controlling defluorination through an appropriate catalyst choice has hitherto prevented this revised sequence from reaching its full potential. However, it is still shown to allow access to the active pharmaceutical ingredient in a stereochemically pure form and has been demonstrated on a multikilogram scale. The reductive aminations in both the original and revised sequences provided different scale-up challenges, and the solutions implemented are described.

BICYCLIC HETEROCYCLE DERIVATIVES HAVING SELECTIVE BACE1 INHIBITORY ACTIVITY

The present invention provides a compound which has an effect of inhibiting amyloid β production, especially an effect of inhibiting selective BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid β proteins. A compound of the formula (IA) or the like, wherein -A1- is alkylene optionally substituted with one or more halogen; R2 is substituted or unsubstituted alkyl or the like; R3 and R4 are each independently a hydrogen atom, halogen, alkyl or haloalkyl or the like; R5 is a hydrogen atom or halogen; A4 is N or CR6 wherein R6 is a hydrogen atom, halogen, or substituted or unsubstituted alkyl; A5 is NR7 or CR8R9; A6 is CR18 or N; R18 is a hydrogen atom; R7 is substituted or unsubstituted alkyl; R8 and R9 are each independently a hydrogen atom, halogen, alkyl or haloalkyl or the like; and Ring B is bicyclic ring; or a pharmaceutically acceptable salt thereof.

INHIBITORS OF DNA GYRASE FOR THE TREATMENT OF BACTERIAL INFECTIONS

The present invention relates to compounds which specifically inhibit bacterial DNA Gyrase and can be used for the treatment of respiratory tract infections.

CARBINOL DERIVATIVES HAVING HETEROCYCLIC LINKER

[Object] It is to provide a novel LXRβ agonist useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate: (wherein, each V and W independently show N or C—R7; each X and Y independently show CH2, C═O, SO2, etc; Z shows CH or N; each R1, R2 and R7 independently show a hydrogen atom, C1-8 alkyl group, etc.; R3 shows C1-8 alkyl group; R4 shows an optionally substituted C6-10 aryl group or an optionally substituted 5- to 11-membered heterocyclic group; R5 and R6 show a hydrogen atom, etc.; L shows a C1-8 alkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.)

The design of efficient and selective routes to pyridyl analogues of 2,3-dihydro-1,4-benzodioxin-6-carbaldehyde

This Letter describes the synthetic routes to challenging pyridyl analogues of 2,3-dihydro-1,4-benzodioxin- 6-carbaldehyde which were key intermediates for our antibacterial medicinal chemistry programme. All routes described started from kojic acid (8) and have been used to give multigram quantities of each aldehyde.

NOVEL NAPHTHYRIDINE DERIVATIVE MONOHYDRATE AND METHOD FOR PRODUCING THE SAME

Disclosed is 1-(2-(4-((2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)amino)piperidin-1-yl)ethyl)-7-fluoro-1,5-naphthyridin-2(1H)-one monohydrate, which has strong antibacterial activity. The compound is highly safe and useful as an original drug for ph

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.

ANTIBACTERIAL AGENTS

2H-chromen-2-one derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.

ANTIBACTERIAL AGENTS

Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.