17335-88-5

Upstream product

• 501-53-1 benzyl chloroformate 
• 142-73-4 iminodiacetic acid 
• 76698-56-1 N-benzyloxycarbonyliminodiacetic acid dicyclohexylamine salt 
• 77-92-9 citric acid 

Downstream Products

• 126765-07-9 [Benzyloxycarbonyl-(2,5-dioxo-pyrrolidin-1-yloxycarbonylmethyl)-amino]-acetic acid 2,5-dioxo-pyrrolidin-1-yl ester 
• 827596-27-0 C₅₈H₉₇N₉O₁₆ 
• 126740-45-2 (2-{Benzyloxycarbonyl-[(methoxycarbonylmethyl-carbamoyl)-methyl]-amino}-acetylamino)-acetic acid methyl ester 
• 100-51-6 benzyl alcohol 
• 123597-24-0 11-<(Benzyloxy)carbonyl>-1'-ethyl-5,17-dimethoxy-4,18-dimethyl-8,11,14-triaza-2,6:16,20-dimethenospiro-9,13-dione 
• 1026940-91-9 {benzyloxycarbonyl-[(2-benzylsulfanyl-ethylcarbamoyl)-methyl]-amino}-acetic acid 2,5-dioxo-pyrrolidin-1-yl ester 
• 1026454-82-9 (benzyloxycarbonyl-{[2-(2-benzylsulfanyl-acetylamino)-ethylcarbamoyl]-methyl}-amino)-acetic acid 
• 1025807-73-1 (2-{benzyloxycarbonyl-[(2-benzylsulfanyl-ethylcarbamoyl)-methyl]-amino}-acetylamino)-acetic acid 
• 145355-43-7 6,10-Dioxo-5,6,7,9,10,11-hexahydro-5,8,11-triaza-benzocyclononene-8-carboxylic acid benzyl ester 
• 105400-47-3 (benzyloxycarbonyl)bis<<(pentafluorophenoxy)carbonyl>methyl>amine 

Relevant academic research and scientific papers

Synthesis and binding properties of hybrid cyclophane - Azamacrocyclic receptors

(Chemical Equation Presented). Three new azamacrocyclic-cyclophane hybrid receptors L1, L2, and L3 have been synthesized that incorporate either 1,4,7,10-tetraazacyclododecane (cyclen) or 1,4,7-triazacyclononane (tacn) uni

Rigid Scaffolds: Synthesis of 2,6-Bridged Piperazines with Functional Groups in all three Bridges

The activity of pharmacologically active compounds can be increased by presenting a drug in a defined conformation, which fits exactly into the binding pocket of its target. Herein, the piperazine scaffold was conformationally restricted by substituted C

Substance related with tophatib and preparation method and application thereof

The invention discloses a substance related with tophatib and a preparation method and application thereof. The substance is named as N,N'-diacetyl{(3R,4R)-4-methyl-3-[methyl(7H-pyrrole[2,3-D]pyrimidine-4-yl)amine]piperidine-1-yl}imine. The impurity is characterized in that the generation level is lower in the condensation reaction process; however, the impurity has the uniform main functional groups with the tophatib, the cleaning effect is limited in the subsequent salting and refining process, and the influence to the qualities of crude drug and finished product of tophatib is larger; by detecting the existence of the impurity, the qualities of the raw material and preparation of the tophatib can be effectively determined.

Large-Scale Synthesis of Piperazine-2,6-dione and Its Use in the Synthesis of Dexrazoxane Analogues

An efficient, large-scale synthesis of piperazine-2,6-dione was developed. The advantages of this procedure include the use of inexpensive starting materials, satisfactory yields, and a convenient workup without the need for chromatographic techniques. Furthermore, this procedure can be easily modified for the preparation of 1-substituted piperazine-2,6-dione hydrobromides. The utility of the prepared piperazine-2,6-dione was demonstrated in the synthesis of a novel analogue of the only drug used in clinical practice to prevent anthracycline-induced cardiotoxicity, dexrazoxane.

TRICYCLIC COMPOUNDS AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS

The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents A, R1, R2, R3a, R3b, R4a, R4b and n are as defined herei

Structure-activity relationships of imidazole-derived 2-[ N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme

Insulin degrading enzyme (IDE) is a zinc metalloprotease that degrades small amyloid peptides such as amyloid-a and insulin. So far the dearth of IDE-specific pharmacological inhibitors impacts the understanding of its role in the physiopathology of Alzheimer's disease, amyloid-a clearance, and its validation as a potential therapeutic target. Hit 1 was previously discovered by high-throughput screening. Here we describe the structure-activity study, that required the synthesis of 48 analogues. We found that while the carboxylic acid, the imidazole and the tertiary amine were critical for activity, the methyl ester was successfully optimized to an amide or a 1,2,4-oxadiazole. Along with improving their activity, compounds were optimized for solubility, lipophilicity and stability in plasma and microsomes. The docking or co-crystallization of some compounds at the exosite or the catalytic site of IDE provided the structural basis for IDE inhibition. The pharmacokinetic properties of best compounds 44 and 46 were measured in vivo. As a result, 44 (BDM43079) and its methyl ester precursor 48 (BDM43124) are useful chemical probes for the exploration of IDE's role.

Synthesis and Anti-herpetic Activity of Phosphoramidate ProTides

Among the many prodrug approaches aimed at delivering nucleoside monophosphates into cells, the phosphoramidate ProTide approach is one that has shown success, which has made it possible for some of the phosphoramidates to enter into clinical trials. Herein, we report the synthesis and antiviral activity of a series of phosphoramidate ProTides designed to bypass the thymidine kinase (TK) dependence of the parent nucleoside analogues. Phosphoramidate derivatives of (E)-5-(2-bromovinyl)-2′-deoxyuridine (BVDU) that contain L-alanine or pivaloyloxymethyl iminodiacetate (IDA-POM) exhibit anti-HSV-1 and anti-VZV activity in cell cultures, but they largely lost antiviral potency against TK-deficient virus strains. Among deazapurine nucleosides and their phosphoramidate derivatives, the 7-deazaadenine containing nucleosides and their phosphoramidate triester derivatives showed weak antiviral activity against VZV. Apparently, intracellular nucleotide delivery with these phosphoramidates is partly successful. However, none of the compound prodrugs showed superior activity to their parent drugs. Copyright

Synthesis and biological evaluation of pyrophosphate mimics of thiamine pyrophosphate based on a triazole scaffold

Novel triazole-based pyrophosphate analogues of thiamine pyrophosphate (TPP) have been synthesised and tested for inhibition of pyruvate decarboxylase (PDC) from Zymomonas mobilis. The thiazolium ring of thiamine was replaced by a triazole in an efficient two-step procedure. Pyrophosphorylation then gave extremely potent triazole inhibitors with KI values down to 20 pM, compared to a KD value of 0.35 μM for TPP. This triazole scaffold was used for further investigation and six analogues containing mimics of the pyrophosphate group were synthesised and tested for inhibition of PDC. Several effective analogues were found with KI values down to around 1 nM.

BUPRENORPHINE DERIVATIVES AND USES THEREOF

Ester derivatives of the phenolic hydroxyl group of buprenorphine are described that can be used in the treatment of opiate dependency and/or moderate to severe pain. The esters have an enhanced bioavailability, an enhanced duration of action, and a reduc

HYDROXY PYRIDOPYRROLOPYRAZINE DIONE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS

Hydroxy-substituted pyridopyrrolopyrazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I): (I) wherein a, b, A, B, R1, R2, R3, R4, R5, R6, R7 and R8 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.