79069-62-8

Upstream product

• 13574-13-5 Boc-Glu(OBzl)-OH 
• 32886-40-1 (S)-2-tert-Butoxycarbonylamino-pentanedioic acid 5-benzyl ester 1-(2,5-dioxo-pyrrolidin-1-yl) ester 
• 56-86-0 L-glutamic acid 
• 24424-99-5 di-tert-butyl dicarbonate 
• 100-51-6 benzyl alcohol 
• 1676-73-9 L-glutamic acid γ-benzyl ester 
• 59279-58-2 N^α-tert-butyloxycarbonyl-γ-benzyloxycarbonyl-L-glutamic acid methyl ester 

Downstream Products

• 299432-52-3 benzyl (4S)-4-(tert-butoxycarbonyl)amino-5-[(2-methoxyethoxy)methoxy]pentanoate 
• 911050-94-7 benzyl (4S)-4-(tert-butoxycarbonyl)amino-5-[(2,2-dimethylpropanoyl)oxy]pentanoate 
• 931396-31-5 5-[allyloxycarbonylmethyl-(2-nitro-benzenesulfonyl)-amino]-4-tert-butoxycarbonylamino-pentanoic acid benzyl ester 
• 849438-12-6 (4S)-tert-butyl 4-(3-benzyloxy-3-oxopropyl)-2,2-dimethyloxazolidine-3-carboxylate 
• 1376616-05-5 (S)-benzyl 5-acetoxy-4-(tert-butoxycarbonyl)aminopentanoate 
• 1376616-07-7 (S)-benzyl 5-acetoxy-4-aminopentanoate 
• 1376616-08-8 (S)-benzyl 5-acetoxy-4-(4-(2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl)benzamido)pentanoate 
• 1376616-09-9 (S)-5-acetoxy-4-(4-(2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl)benzamido)pentanoic acid 
• 1429399-41-6 C₁₇H₂₄INO₄ 
• 1429399-43-8 Boc-γ³-Cys(Ac)-OBn 
• 1429399-45-0 H-α-CyE(Boc,OBn)-OEt 

Relevant academic research and scientific papers

RETRACTED ARTICLE: Asymmetric Synthesis of Apratoxin e

An efficient method for asymmetric synthesis of apratoxin E 2 is described in this report. The chiral lactone 8, recycled from the degradation of saponin glycosides, was utilized to prepare the non-peptide fragment 6. In addition to this "from nature to nature" strategy, olefin cross-metathesis (CM) was applied as an alternative approach for the formation of the double bond. Moreover, pentafluorophenyl diphenylphosphinate was found to be an efficient condensation reagent for the macrocyclization.

Method for preparing (S)-4-amino-5-mercaptopentanoic acid

The invention belongs to the technical field of medicines, and relates to a simple method for preparing (S)-4-amino-5-mercaptopentanoic acid with potential medicinal application values. The method is characterized in that an amino group and a gamma-carbox

A multifaceted secondary structure mimic based on piperidine-piperidinones

Minimalist secondary structure mimics are typically made to resemble one interface in a protein-protein interaction (PPI), and thus perturb it. We recently proposed suitable chemotypes can be matched with interface regions directly, without regard for secondary structures. Here we describe a modular synthesis of a new chemotype 1, simulation of its solution-state conformational ensemble, and correlation of that with ideal secondary structures and real interface regions in PPIs. Scaffold 1 presents amino acid side-chains that are quite separated from each other, in orientations that closely resemble ideal sheet or helical structures, similar non-ideal structures at PPI interfaces, and regions of other PPI interfaces where the mimic conformation does not resemble any secondary structure. 68 different PPIs where conformations of 1 matched well were identified. A new method is also presented to determine the relevance of a minimalist mimic crystal structure to its solution conformations. Thus dld-1-faf crystallized in a conformation that is estimated to be 0.91 kcal-mol-1 above the minimum energy solution state. Do we know, when designing a new peptidomimetic scaffold like the one shown, how it can resemble secondary structures? Design and modular synthesis of this elongated mimic is reported, and the structure is related to ideal and real structures at PPI interfaces.

DRUG DERIVATIVES

The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives). In other cases, the oxidation state of the derivative of the invention may be regarded as being different from that of the parent compound. In many cases, the compounds of the invention have inherent therapeutic activity on their own account. In some cases, this activity relative to the same target or targets of the parent compound is as good as or better than the activity which the parent compound has against the target or targets.

Novel thiol- and thioether-containing amino acids: Cystathionine and homocysteine families

Natural l-homocysteine and l,l-cystathionine, along with a series of unnatural analogues, have been prepared from l-aspartic and l-glutamic acid. Manipulation of the protected derivatives provided ω-iodoamino acids, which were used in thioalkylation react

DRUG DERIVATIVES

The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives). In other cases, the oxidation state of the derivative of the invention may be regarded as being different from that of the parent compound. In many cases, the compounds of the invention have inherent therapeutic activity on their own account. In some cases, this activity relative to the same target or targets of the parent compound is as good as or better than the activity which the parent compound has against the target or targets.

CATHEPSIN CYSTEINE PROTEASE INHIBITORS

The present invention relates to novel compounds of the formula (I), wherein R'-R7, X, Y, D and n are as defined in the specification. These compounds are cysteine protease inhibitors which include but are not limited to inhibitors of cathepsms K, L, S an

A new diastereoselective synthetic approach to the enantiopure peptidomimetic scaffold 2-oxo-1-azabicyclo[4.4.0]decane

A general method for the synthesis of unsubstituted and C-7-substituted azabicyclo[4.4.0]decane dipeptides (23, 30a, and 30b) that can serve as dipeptide mimetics has been developed. The key step of this new method involves the coupling reaction of the ox

Synthesis and neuroprotective activity of analogues of glycyl-L-prolyl-L- glutamic acid (GPE) modified at the α-carboxylic acid

The synthesis of nine GPE* analogues, wherein the α-carboxylic acid group of glutamic acid has been modified, is described by coupling readily accessible N-benzyloxycarbonyl-glycyl-l-proline 2 with various analogues of glutamic acid. Pharmacological evaluation of the novel compounds was undertaken to further understand the role of the glutamate residue on the observed neuroprotective properties of the endogenous tripeptide GPE.