84348-41-4

Usage

Uses

Used in Pharmaceutical Industry:
(S)-methyl 4-methylenepyrrolidine-2-carboxylate hydrochloride is used as a synthetic intermediate for the production of various drugs, including anti-psychotic and anti-depressant medications. Its role in the synthesis process is crucial for creating effective treatments for mental health disorders.
Used in Chemical Synthesis:
(S)-methyl 4-methylenepyrrolidine-2-carboxylate hydrochloride is also used as a building block in the chemical synthesis of other complex molecules, contributing to the development of a diverse range of pharmaceutical products. Its versatility in chemical reactions makes it a valuable component in the creation of new and innovative medications.

Upstream product

• 84348-40-3 methyl 4-methylene-L-proline 
• 84348-38-9 (S)-1-(tert-butoxycarbonyl)-4-methylenepyrrolidine-2-carboxylic acid 
• 84348-39-0 (S)-1-tert-butyl 2-methyl 4-methylenepyrrolidine-1,2-dicarboxylate 
• 79-37-8 oxalyl dichloride 
• 57-50-1 Sucrose 
• 67-56-1 methanol 

Downstream Products

• 200184-60-7 (S)-N-benzyloxycarbonyl-4-methylenepyrrolidine-2-carboxylic acid methyl ester 
• 1173715-82-6 methyl (2S)-4-methylene-1-p-toluenesulfonylpyrroplidine-2-carboxylate 
• 1094039-81-2 (2S)-methyl N-benzoyl-4-methylenepyrrolidine-2-carboxylate 
• 232931-61-2 [4-[3-[4-[(2S)-2-(hydroxymethyl)-4-methylene-pyrrolidine-1-carbonyl]-2-methoxy-5-nitrophenoxy]propoxy]-5-methoxy-2-nitro-phenyl]-[(2S)-2-(hydroxymethyl)-4-methylene-pyrrolidin-1-yl]methanone 
• 232931-60-1 [4-[3-[4-[(2S)-2-[[tert-butyl(dimethyl)silyl]oxymethyl]-4-methylenepyrrolidine-1-carbonyl]-2-methoxy-5-nitrophenoxy]propoxy]-5-methoxy-2-nitrophenyl]-[(2S)-2-[[tert-butyl(dimethyl)silyl]oxymethyl]-4-methylene-pyrrolidin-1-yl]methanone 

Relevant academic research and scientific papers

NOVEL CONNECTED BODY AND USE THEREOF IN SPECIFIC CONJUGATION BETWEEN BIOMOLECULE AND DRUG

PROBLEM TO BE SOLVED: To provide: a method for producing a connected body; a method for using the connected body in the production of a uniform conjugate; and a method for applying the conjugate in the treatment of cancer, infectious diseases, and autoimmune diseases. SOLUTION: A novel connected body is provided that includes a 2,3-di-substituted succinic acid group or a 2-mono-substituted or 2,3-di-substituted fumaric acid or maleic acid (trans (E)- or cis (Z)-butenedioic acid) group for conjugating 2 or more compounds/cytotoxic agents per connected body with a cell-binding molecule by specifically bridge-linking to a pair of thiol on the cell-binding molecule. The connected body is exemplified by the following general formula. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT

VISUAL DETECTION OF PBD INDUCED DNA CROSSLINKS

The present invention relates to the field of oncology, laboratory tools and methods, and especially anti-tumor DNA crosslinking agents. Most patients with advanced solid tumors develop resistance to chemotherapy due to the ability of cancer cells to repair or tolerate sustained DNA damages. The inventors showed that the compounds according to the present invention allow the detection and visualization of alkylated DNA damages induced by PBDs without altering their DNA crosslinking ability. This enables the study of the effect and properties of PBDs. In particular, the present invention relates new derivates of PBD molecules and their synthesis. The present invention also relates to a method for visualizing DNA crosslinking; to a method for assessing the resistance of a tumor to a crosslinking agent and to a method for identifying a molecule or treatment for improving the efficiency of a crosslinking agent.

CROSS-LINKED PYRROLOBENZODIAZEPINE DIMER (PBD) DERIVATIVE AND ITS CONJUGATES

A novel cross-linked cytotoxic agents, pyrrolobenzo-diazepine dimer (PBD) derivatives, and their conjugates to a cell-binding molecule, a method for preparation of the conjugates and the therapeutic use of the conjugates.

CONJUGATION LINKERS CONTAINING 2,3-DIAMINOSUCCINYL GROUP

Provided is a conjugate of a cytotoxic drug/molecule to a cell-binding molecule with a bis-linker (adual-linker) containing a 2, 3-diaminosuccinyl group. It also relates to preparation of the conjugate of a cytotoxic drug/molecule to a cell-binding molecule with the bis-linker, particularly when the drug having functional groups of amino, hydroxyl, diamino, amino-hydroxyl, dihydroxyl, carboxyl, hydrazine, aldehyde and thiol for conjugation with the bis-linker in a specific manner, as well as the therapeutic use of the conjugates.

PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF

Conjugates and compounds for making conjugates which are PBD molecules linked via the N10 position are disclosed, along with the use of the conjugates for treating proliferative diseases, including cancer.

PYRROLOBENZODIAZEPINE CONJUGATES

A compound of formula (I) : (I) and its conjugates.

CONJUGATION LINKERS, CELL BINDING MOLECULE-DRUG CONJUGATES CONTAINING THE LIKERS, METHODS OF MAKING AND USES SUCH CONJUGATES WITH THE LINKERS

The present invention relates to linkers having a group of propiolyl, substituted acryl (acryloyl), or disubstituted propanoyl, and using such linkers for the conjugation of compounds, in particular, cytotoxic agents to a cell-binding molecule.

PYRROLOBENZODIAZEPINE CONJUGATES

A conjugate of formula (I), wherein L is a Ligand unit, D is a Drug Linker unit of formula (II), wherein either: (a) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (b)

PYRROLOBENZODIAZEPINE CONJUGATES

A conjugate of formula (I): L - (DL)p (I) wherein L is a Ligand unit, D is a Drug Linker unit of formula (II) wherein p is an integer of from 1 to 20.

PYRROLOBENZODIAZEPINE ANTI-HER2 ANTIBODY CONJUGATES

A conjugate of formula (I) L - (DL)p (I) wherein L is an antibody (Ab) which binds HER2, D is a Drug Linker unit of formula (A) wherein p is an integer of from 1 to 20.