56441-97-5

Usage

Uses

Used in Pharmaceutical Industry:
METHYL 4-BENZYLOXY-3-METHOXYBENZOATE is used as an intermediate in the synthesis of Clomiphene (C587025), a synthetic estrogen agonist-antagonist. It plays a vital role in the production of this medication, which is primarily used to treat infertility in women by stimulating ovulation. METHYL 4-BENZYLOXY-3-METHOXYBENZOATE's structural properties allow it to participate in various chemical reactions, facilitating the synthesis of Clomiphene and other related pharmaceuticals.

Upstream product

• 3943-74-6 4-hydroxy-3-methoxybenzoic acid methyl ester 
• 100-44-7 benzyl chloride 
• 100-39-0 benzyl bromide 
• 1486-53-9 4-(benzyloxy)-3-methoxybenzoic acid 
• 74-88-4 methyl iodide 
• 67-56-1 methanol 
• 2426-87-1 3-methoxy-4-(phenylmethoxy)benzaldehyde 
• 121-33-5 vanillin 
• 121-34-6 3-methoxy-4-hydroxybenzoic acid 

Downstream Products

• 51908-43-1 1-(4-Benzyloxy-3-methoxy-phenyl)-2-methanesulfonyl-ethanone 
• 61032-41-5 methyl 4-(benzyloxy)-5-methoxy-2-nitrobenzoate 
• 3943-74-6 4-hydroxy-3-methoxybenzoic acid methyl ester 
• 51908-42-0 1,4-Bis-(4-benzyloxy-3-methoxy-phenyl)-butane-1,4-dione 
• 51908-39-5 1,4-Bis-(4-benzyloxy-3-methoxy-phenyl)-2-methanesulfonyl-butane-1,4-dione 
• 1447973-63-8 C₁₆H₁₆O₅ 
• 144216-37-5 4-hydroxy-3-methoxy-benzohydroxamic acid 

Relevant academic research and scientific papers

COMPOSITIONS AND METHODS RELATED TO MOLECULAR CONJUGATION

The invention relates to activated Michael acceptor (AMA) compounds that can undergo conjugation with biomolecules containing Michael donor moieties, thereby providing plasma-stable antibody-drug conjugates (ADCs). Pharmaceutical compositions of the ADCs are disclosed as well. Also provided herein are a number of applications (e.g., therapeutic applications) in which the compositions are useful.

Transition Metal-Free Regioselective Remote C?H Bond 2,2,2-Trifluoroethoxylation of 8-Aminoquinoline Derivatives at the C5 Position

The regioselective 2,2,2-trifluoroethoxylation at the C5 position of amides derived from the 8-aminoquinoline has been developed. In the presence of PIDA, an unprecedented and undirected transition metal-free transformation was achieved using the readily available and appealing 2,2,2-trifluoroethanol as the fluorinated source. The selective distal 2,2,2-trifluoroethoxylation of an array of amides was achieved in moderate to good yields (12 examples, up to 61 % yield). This approach provided efficient access to high-value added fluorinated quinoline derivatives, key building blocks for bulk and fine chemical industry.

FUSED HETEROCYCLIC BENZODIAZEPINE DERIVATIVES AND USES THEREOF

The present disclosure provides compounds and compositions capable of extending lifespan, and methods of use thereof.

Structure–activity relationship study of novel quinazoline-based 1,6-naphthyridinones as MET inhibitors with potent antitumor efficacy

As a privileged scaffold, the quinazoline ring is widely used in the development of EGFR inhibitors, while few quinazoline-based MET inhibitors are reported. In our ongoing efforts to develop new MET-targeted anticancer drug candidates, a series of quinaz

Heterocyclic compound, preparation method and application thereof

The invention relates to a heterocyclic compound in the technical field of medicines. The compound is represented by a structural general formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, X, Y, Z, Cy1, Cy2, m, n and t have the meanings given in the specification; in addition, the invention also discloses an application of the compound and the pharmaceuticallyacceptable salt thereof in preparation of drugs for treating diseases caused by abnormal high expression of tyrosine kinase, especially application in preparation of drugs for treating and preventingcancers.

NOVEL BENZODIAZEPINE DERIVATIVES AND USES THEREOF

The present disclosure provides compounds and compositions capable of extending lifespan, and methods of use thereof.

Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962)

Herein, we report the discovery of a new, orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 (mGlu7) negative allosteric modulator (NAM) that achieves exposure in cerebral spinal fluid (CSF) 2.5× above the in vitro IC50 at minimum effective doses (MEDs) of 3 mg/kg in preclinical anxiety models.

METHODS OF PREPARING INDOLINOBENZODIAZEPINE DERIVATIVES

The invention provides novel methods for preparing indolinobenzodiazepine monomer compounds and their synthetic precursors.

Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti-Plasmodium activity

Plasmodium falciparum HKMTs (PfHKMTs) play a key role in controlling Plasmodium gene expression and represent exciting new anti-malarial epigenetic targets. Using an inhibitor series derived from the diaminoquinazoline HKMT inhibitory chemotype, we have previously identified compounds with highly promising antimalarial activity, including irreversible asexual cycle blood stage-independent cytotoxic activity at nM concentrations, oral efficacy in in vivo models of disease, and the unprecedented ability to reactivate dormant liver stage parasites (hypnozoites). However, future development of this series will need to address host versus parasite selectivity, where inhibitory activity against human G9a is removed from the lead compounds, while maintaining potent anti-Plasmodium activity. Herein, we report an extensive study of the SAR of this series against both G9a and P. falciparum. We have identified key SAR features which demonstrate that high parasite vs. G9a selectivity can be achieved by selecting appropriate substituents at position 2, 4 and 7 of the quinazoline ring. We have also, in turn, discovered that potent G9a inhibitors can be identified by employing a 6-carbon 'Nle mimic' at position 7. Together, this data suggests that while broadly similar, the G9a and potential PfHKMT target(s) binding pockets and/or binding modes of the diaminoquinazoline analogues exhibit clear and exploitable differences. Based on this, we believe this scaffold to have clear potential for development into a novel anti-malarial therapeutic.

PYRROLOBENZODIAZEPINE ANTIBODY DRUG CONJUGATES AND METHODS OF USE

The invention provides antibody-drug conjugates comprising an antibody conjugated to a pyrrolobenzodiazepine drug moiety via a disulfide linker, pyrrolobenzodiazepine linker-drug intermediates, and methods of using the antibody-drug conjugates.