73236-85-8

Upstream product

• 128542-75-6 (S)-2-(bromomethyl)-1-<(tert-butyloxy)carbonyl>pyrrolidine 
• 10387-40-3 potassium thioacetate 
• 86661-32-7 (S)-tert-butyl 2-((tosyloxy)methyl)pyrrolidine-1-carboxylate 
• 56827-86-2 cesium thioacetate 
• 507-09-5 tiolacetic acid 
• 69610-40-8 N-(tert-butoxycarbonyl)-L-prolinol 
• 2577-48-2 methyl (2S)-pyrrolidine carboxylate 
• 59936-29-7 (S)-N-(tert-butoxycarbonyl)proline methyl ester 
• 147-85-3 L-proline 
• 24424-99-5 di-tert-butyl dicarbonate 
• 132482-09-8 tert-butyl (2S)-2-{[(methylsulfonyl)oxy]methyl}-pyrrolidine-1-carboxylate 
• 23356-96-9 (S)-1-Pyrrolidin-2-yl-methanol 

Downstream Products

• 188625-66-3 (S)-2-(mercaptomethyl)-1-<(tert-butyloxy)carbonyl>pyrrolidine 

Relevant academic research and scientific papers

AMINOPYRIDINE COMPOUNDS AND METHODS FOR THE PREPARATION AND USE THEREOF

The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A/B (Rgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I and Formula III, as described herein, and pharmaceutically acceptable salts thereof.

Design and synthesis of water soluble β-aminosulfone analogues of SCH 900229 as γ-secretase inhibitors

In this paper we describe our strategy to improve the aqueous solubility of SCH 900229, a potent PS1-selective γ-secretase inhibitor for the treatment of Alzheimer's disease. Incorporation of ionizable amino groups into the side chain terminal generates w

Chemical synthesis of N-peptidyl 2-pyrrolidinemethanethiol for peptide ligation

Peptides carrying a C-terminal 2-pyrrolidinemethanethiol (PMT) unit were synthesized using 9-fluorenylmethoxycarbonyl (Fmoc) solid-phase peptide synthesis (SPPS), and were shown to ligate efficiently with cysteinyl-peptides. This novel PMT-mediated ligation tolerated many different C-terminal residues and was successfully applied to a one-pot N-to-C sequential ligation reaction and the semi-synthesis of lysine 16 acetylated histone H4, demonstrating the utility of the method in peptide and protein synthesis.

GAMMA SECRETASE INHIBITORS

Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing t

Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors

Potent SAH analogues with constrained homocysteine units have been designed and synthesized as inhibitors of human DNMT enzymes. The five membered (2S,4S)-4-mercaptopyrrolidine-2-carboxylic acid, in 1a, was a good replacement for homocysteine, while the corresponding six-member counterpart was less active. Further optimization of 1a, changed the selectivity profile of these inhibitors. A Chloro substituent at the 2-position of 1a, compound 1d, retained potency against DNMT1, while N6 alkylation, compound 7a, conserved DNMT3b2 activity. The concomitant substitutions of 1a at both 2- and N6 positions reduced activity against both enzymes.

The synthesis of a new class of oxytocin antagonists

The synthesis of a new class of oxytocin antagonists, with significantly modified C-terminal part, is described. The chemistry of the Mitsunobu reaction was applied to obtain the key derivatives. In spite of the extensive modifications of previously described compound F792, the peptides retain biological activity as oxytocin antagonists.

Synthesis of chiral β-amino sulfides and β-amino thiols from α-amino acids

Bifurcated routes to two series of chiral secondary β-amino sulfides 5a-c and 11a-c have been developed from L-proline and (S)-phenylglycine, respectively. The developed methodology had also led to the synthesis of the tertiary β-amino thiol 7 and the primary β-amino sulfide 12 from L-proline and (S)-phenylglycine, respectively.

Homodimeric and heterodimeric bis(amino thiol) oxometal complexes with rhenium(V) and technetium(V). Control of heterodimeric complex formation and an approach to metal complexes that mimic steroid hormones

We have investigated the possibility of preparing complexes of rhenium and technetium whose shape resembles that of ligands for steroid receptors. The general structure of N2S2 complexes of oxorhenium(V) and oxotechnetium(V) is such that they could replace the BC ring system of steroid, thereby generating a metal complex system with considerable size and shape similarity to a steroid. Such a metal-integrated steroid-shaped complex can be constructed as a heterodimer of two different amino thiols; complexes of rhenium and technetium with such heterodimeric bis-bidentate structure have not been systematically studied. In this investigation, we have shown that complexes of this nature form readily when appropriate metal precursors are combined with a mixture of amino thiols. In the systems we have studied, heterodimeric complex formation is preferred over homodimeric complex formation, and in one system where we were able to obtain an X-ray crystal structure, this oxorhenium heterodimer had the desired trans geometry. These rhenium and technetium-99m complexes are reasonably stable toward ligand exchange; they can be readily purified by chromatography under appropriate conditions, and the one technetium-99m complex studied in vivo shows some persistence in blood and gives good initial uptake in several tissues. The convenient and selective formation of such bis-bidentate heterodimeric complexes suggests that the development of metal-integrated complexes that resemble ligands for receptors may be possible.

2-thiomethyl-substituted-1,4-dihydropyridines, method for their preparation and pharmaceutical compositions containing them

Compounds of formula I STR1 wherein R1 is an alkoxycarbonyl group, acetyl, benzoyl, cyano, nitro or aminocarbonyl; R2 is an optionally substituted aryl or hetaryl group; R3 is an alkoxycarbonyl group; φ is a thio residue such as alkylthio, cycloalkylthio, arylthio, heteroarylthio, aminoalkylthio, are described. Compounds I are useful in human therapy as antihypertensive, antiulcer, antithrombotic, antiischaemic agents.