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Usage

Uses

Used in Pharmaceutical Industry:
BOC-L-ASPARTIMOL T-BUTYL ESTER is used as a building block for the preparation of peptide-based drugs and pharmaceuticals. Its role in this industry is pivotal due to its ability to protect the reactive functional groups during the synthesis process, which is essential for creating stable and effective peptide-based medications.
Used in Organic Synthesis:
In the field of organic synthesis, BOC-L-ASPARTIMOL T-BUTYL ESTER is utilized as a protected form of aspartic acid. It is used to facilitate chemical reactions by safeguarding the reactive functional groups, thereby enhancing the efficiency and success of peptide and peptidomimetic synthesis.
Used in Peptide Synthesis:
BOC-L-ASPARTIMOL T-BUTYL ESTER is employed as a protecting agent in peptide synthesis. Its function is to shield the carboxyl group of aspartic acid, allowing for the controlled formation of peptide bonds without unwanted side reactions, which is crucial for the synthesis of complex peptide structures.
Used in Peptidomimetic Synthesis:
BOC-L-ASPARTIMOL T-BUTYL ESTER is also used in the synthesis of peptidomimetics, which are compounds that mimic the structure and function of peptides. Here, it serves to protect the functional groups during the synthesis, enabling the creation of novel bioactive molecules with potential therapeutic applications.

InChI:InChI=1/C13H25NO5/c1-12(2,3)18-10(16)7-9(8-15)14-11(17)19-13(4,5)6/h9,15H,7-8H2,1-6H3,(H,14,17)/t9-/m0/s1

Upstream product

• 18635-49-9 4-tert-butyl 1-methyl L-N-(tert-butoxycarbonyl)aspartate 
• 1676-90-0 Boc-Asp(OtBu)-OH 
• 543-27-1 isobutyl chloroformate 
• 1913-12-8 β-tert-butyl-N-(tert-butoxycarbonyl)-L-aspartic acid dicyclohexylammonium salt 
• 3057-74-7 L-Asp(t-Bu) 
• 24424-99-5 di-tert-butyl dicarbonate 
• 50715-50-9 O¹-(2,5-dioxopyrrolidin-1-yl)-O⁴-tert-butyl-(2S)-2-(tert-butoxycarbonylamino)-butanedioate 

Downstream Products

• 220542-06-3 tert-butyl 3(S)-(tert-butoxycarbonylamino)-4-(p-tolylsulfonyloxy)butanoate 
• 911635-43-3 3-t-butoxycarbonylamino-4-(5,5-difluoro-2-oxo-piperidin-1-yl)butyric acid 
• 1393721-13-5 (S)-tert-butyl 4-(benzyl(methyl)amino)-3-(tert-butoxycarbonylamino)butanoate 
• 1802736-56-6 (3S)-3-[(tert-butoxycarbonyl)amino]-4-iodobutanoic acid tert-butyl ester 
• 1246261-58-4 Z-Val-Asp(β-tert-butyl)vinyl methylsulfone 

Relevant academic research and scientific papers

Synthesis and evaluation of L-cystathionine as a standard for amino acid analysis

L-Cystathionine is a key nonprotein amino acid related to metabolic conditions. The quantitative determination of L-cystathionine in physiological fluids by amino acid analysis is important for clinical diagnosis; however, certified reference material for L-cystathionine with satisfactory purity, content, and quantity has been unavailable until recently. Consequently, a practical and simple method for the preparation of L-cystathionine was examined, which involves thioalkylation of N-tert-butoxycarbonyl-Lcysteine tert-butyl ester, derived from L-cystine, with (2S)-2-(tert-butoxycarbonyl)amino-4-iodobutanoic acid tert-butyl ester, derived from L-aspartic acid, to obtain L-cystathionine with protecting groups, followed by single-step deprotection under mild conditions. This method produces L-cystathionine in high purity (99.4%) and having sufficient percentage content according to amino acid analysis, which could be used as a standard for the amino acid analysis of physiological fluids.

Synthesis and Biochemical Evaluation of Biotinylated Conjugates of Largazole Analogues: Selective Class I Histone Deacetylase Inhibitors

The synthesis of biotinylated conjugates of synthetic analogues of the potent and selective histone deacetylase (HDAC) inhibitor largazole is reported. The thiazole moiety of the parent compound's cap group was derivatized to allow the chemical conjugation to biotin. The derivatized largazole analogues were assayed across a panel of HDACs 1–9 and retained potent and selective inhibitory activity towards the class I HDAC isoforms. The biotinylated conjugate was further shown to pull down HDACs 1, 2, and 3.

Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles

Natural, nonribosomal cyclotetrapeptides have traditionally been a rich source of inspiration for design of potent histone deacetylase (HDAC) inhibitors. We recently disclosed the total synthesis and full HDAC profiling of the naturally occurring azumamides (J. Med. Chem. 2013, 56, 6512). In this work, we investigate the structural requirements for potent HDAC inhibition by macrocyclic peptides using the azumamides along with a series of unnatural analogues obtained through chemical synthesis. By solving solution NMR structures of selected macrocycles and combining these findings with molecular modeling, we pinpoint crucial enzyme-ligand interactions required for potent inhibition of HDAC3. Docking of additional natural products confirmed these features to be generally important. Combined with the structural conservation across HDACs 1-3, this suggests that while cyclotetrapeptides have provided potent and class-selective HDAC inhibitors, it will be challenging to distinguish between the three major class I deacetylases using these chemotypes.

Method for producing pyrazole derivative

PROBLEM TO BE SOLVED: To provide a method for producing a pyrazole derivative. SOLUTION: There is provided the method for producing a pyrazole derivative by using a compound represented by formula (IIC), (IID) or (III) and a compound represented by formula (IV). SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT

PYRAZOLE DERIVATIVE, OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF

[Problem] The present invention is to provide a novel pyrazole derivative, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and a pharmaceutical use thereof. [Solution] The present invention provides a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof, which has TRPM8 inhibitory effects: wherein ring A is C6-10 aryl or the like; X is CR4a or the like; R1 and R2 are a hydrogen atom or the like; R3 is a hydrogen atom or the like; R4 is a hydrogen atom or the like; ring B is C6-10 aryl or the like; R5 is a hydrogen atom or the like; R6a is a hydrogen atom or the like; R7a is a hydrogen atom or the like; R7b is a hydrogen atom or the like; R6b is a hydrogen atom or the like; R8 is a hydrogen atom or the like; n is 0, 1 or 2. Therefore, the compound represented by the formula (I) of the present invention or a pharmaceutically acceptable salt thereof is useful as an agent for treating or preventing diseases or symptoms caused by hyperexcitability or disorder of afferent neurons.

Selective caspase inhibitors and uses thereof

The present invention relates to compounds of Formula I, IA, II, HA, III, or IHA and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, IA, II, IIA, III, or IIIA are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases).

BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS AND USES THEREOF

β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

HETEROARYL BUTANOIC ACID DERIVATIVES AS LTA4H INHIBITORS

The present invention describes novel heteroaryl butanoic acid derivatives that are in particular inhibitors of leukotriene A4 hydrolase (LTA4H). The present invention also relates to pharmaceutical compositions comprising said novel heteroaryl butanoic acid derivatives, methods of using said compounds in the treatment of various diseases and disorders, and processes for preparing the said novel compounds.

Novel heteroaryl butanoic acid derivatives

The present invention describes novel heteroaryl butanoic acid derivatives that are good drug candidates especially with regard to leukotriene A4 hydrolase (LTA4H). The present invention also relates to pharmaceutical compositions comprising said novel he

BETA-AMIMO PATEAMINE A DERIVATIVES AND METHODS FOR TREATING CHRONIC LYMPHOCYTIC LEUKEMIA

Pateamine A derivatives, pharmaceutical compositions that include the derivatives, and methods for treating chronic lymphocytic leukemia using the derivatives.