861657-91-2

Usage

Uses

Used in Pharmaceutical Industry:
Methyl 1-Boc-5-oxopyrrolidine-2-carboxylate is used as a building block in the synthesis of pharmaceuticals and other organic compounds. Its presence of the Boc protecting group allows for the selective protection of amines during organic synthesis, enabling the formation of complex molecules with specific functional groups.
Used in Organic Synthesis:
Methyl 1-Boc-5-oxopyrrolidine-2-carboxylate is used as a versatile intermediate in organic synthesis for the preparation of various organic compounds. The Boc protecting group can be selectively removed under mild conditions, allowing for further functionalization and modification of the molecule.
It is important to handle and store Methyl 1-Boc-5-oxopyrrolidine-2-carboxylate with care, following appropriate safety protocols due to its potential hazards and toxicity.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 4931-66-2 methyl 5-oxopyrrolidine-2-carboxylate 
• 145681-01-2 (+/-)-N-tert-butoxycarbonylproline methyl ester 
• 67-56-1 methanol 
• 149-87-1 Pyroglutamic acid 
• 4931-66-2 methyl (S)-pyroglutamate 

Downstream Products

• 195311-23-0 methyl 5-methylpyrrolidine-2-carboxylate 
• 195311-23-0 methyl (2R*,5R*)-5-methylpyrrolidine-2-carboxylate 
• 158706-46-8 (2S/R,5R/S)-1-(tert-butoxycarbonyl)-5-phenylpyrrolidine-2-carboxylic acid 
• 1822538-74-8 1-(tert-butyl) 2-methyl 5-hydroxypiperidine-1,2-dicarboxylate 
• 896731-57-0 C₁₈H₂₂N₂O₅ 
• 170491-63-1 N-Boc-prolinol 
• 861658-15-3 1,5-dimethyl 2-[(t-butoxycarbonyl)amino]pentanedioate 

Relevant academic research and scientific papers

PEPTIDOMIMETIC N5-METHYL-N2-(NONANOYL-L-LEUCYL)-L-GLUTAMINATE DERIVATIVES, TRIAZASPIRO[4.14]NONADECANE DERIVATIVES AND SIMILAR COMPOUNDS AS INHIBITORS OF NOROVIRUS AND CORONAVIRUS REPLICATION

Peptidomimetic N5-methyl-N2-(nonanoyl-L-leucyl)-L-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds for use in methods of inhibiting the replication of noroviruses and coronaviruses in a biological sample or patient, for use in reducing the amount of noroviruses or coronaviruses in a biological sample or patient, and for use in treating norovirus and coronavirus in a patient, comprising administering to said biological sample or patient a safe and effective amount of a compound represented by formulae I or II, or a pharmaceutically acceptable salt thereof. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. page 99 to page 271; examples 1 to 3; compounds A1 to A104 and Bl to B66; tables A to E).

Hydrogen-Borrowing Alkylation of 1,2-Amino Alcohols in the Synthesis of Enantioenriched γ-Aminobutyric Acids

For the first time we have been able to employ enantiopure 1,2-amino alcohols derived from abundant amino acids in C?C bond-forming hydrogen-borrowing alkylation reactions. These reactions are facilitated by the use of the aryl ketone Ph*COMe. Racemisation of the amine stereocentre during alkylation can be prevented by the use of sub-stoichiometric base and protection of the nitrogen with a sterically hindered triphenylmethane (trityl) or benzyl group. The Ph* and trityl groups are readily cleaved in one pot to give γ-aminobutyric acid (GABA) products as their HCl salts without further purification. Both steps may be performed in sequence without isolation of the hydrogen-borrowing intermediate, removing the need for column chromatography.

Design and Synthesis of 56 Shape-Diverse 3D Fragments

Fragment-based drug discovery is now widely adopted for lead generation in the pharmaceutical industry. However, fragment screening collections are often predominantly populated with flat, 2D molecules. Herein, we describe a workflow for the design and synthesis of 56 3D disubstituted pyrrolidine and piperidine fragments that occupy under-represented areas of fragment space (as demonstrated by a principal moments of inertia (PMI) analysis). A key, and unique, underpinning design feature of this fragment collection is that assessment of fragment shape and conformational diversity (by considering conformations up to 1.5 kcal mol?1 above the energy of the global minimum energy conformer) is carried out prior to synthesis and is also used to select targets for synthesis. The 3D fragments were designed to contain suitable synthetic handles for future fragment elaboration. Finally, by comparing our 3D fragments with six commercial libraries, it is clear that our collection has high three-dimensionality and shape diversity.

2-PYRROLIDINE PHENYLHYDRAZIDES ANTIBACTERIAL AGENTS

2-Pyrrolidine phenylhydrazides antibacterial agents The present invention relates to 2-pyrrolidine phenylhydrazide compounds of formula (I), which are selective antibacterials specifically agalnstAcineto barter baumannii.The invention also relates to their therapeutic use as antibacterials, to a process for their preparation and to pharmaceutical compositions containing them.

Preparation method for tert-butyl dioxy-3,8-diazabicyclo[3.2.1]octane-8-carboxylic acid

The invention relates to a preparation method for tert-butyl dioxy-3,8-diazabicyclo[3.2.1]octane-8-carboxylic acid, and mainly solves the technical problems that in an existing synthetic process, the yield is low, the reaction is not easy to control, the experimental operation is inconvenient and the like. By taking t-butyloxycarboryl methyl pyroglutamate as an initial raw material, the tert-butyl dioxy-3,8-diazabicyclo[3.2.1]octane-8-carboxylic acid is prepared by five-step reactions. The tert-butyl dioxy-3,8-diazabicyclo[3.2.1]octane-8-carboxylic acid obtained by the method provided by the invention is a useful intermediate or an intermediate product for synthesis of multiple drugs.

FUSED RING COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

Provided are fused tricyclic compounds effective to inhibit the function of the NS5A protein of formula (I), wherein X, X', Y, Y', A, A',Q1, Q2, R1-R4, X4, R5a, f and W are defined as in the description. Also provided herein are pharmaceutical compositions thereof, and uses in the manufacture of a medicament for treating HCV infection or a HCV disorder thereof.

Oxidative transformation of cyclic ethers/amines to lactones/lactams using a DIB/TBHP protocol

A novel C-H oxidation of cyclic ethers and amines to the corresponding lactones and lactams was developed using a DIB/TBHP protocol. The reaction is mild and no metallic reagent is involved. In addition, study shows that the electronic properties of the substituents could affect the selectivity of oxidation. The Royal Society of Chemistry 2013.

Novel Receptor Antagonists and Their Methods of Use

The present invention relates to novel oxo-prolinamide derivatives of formula (I) which modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.

2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists

A series of 2,5-cis-disubstituted pyrrolidines were synthesized and evaluated as S1P receptor agonists. Compounds 15-21 were identified with good selectivity over S1P3 which lowered circulating lymphocytes after oral administration in mice.

Cathepsin cysteine protease inhibitors

This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of Cathepsins K and L. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.