152120-54-2

Usage

Uses

Used in Pharmaceutical Industry:
N,N'-BIS-BOC-1-GUANYLPYRAZOLE is used as a guanidinylating reagent for the stereoselective synthesis of bicyclic guanidine alkaloids, such as (+)-monanchorin. This application is significant in the development of new pharmaceutical compounds with potential therapeutic properties.
Used in Organic Synthesis:
In the field of organic synthesis, N,N'-BIS-BOC-1-GUANYLPYRAZOLE serves as an essential reagent for the synthesis of complex organic molecules, particularly those containing guanidine functional groups. Its use in this industry is vital for the creation of novel chemical entities with potential applications in various sectors, including pharmaceuticals, agrochemicals, and materials science.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 152120-61-1 tert-butyl (1H-pyrazol-1-ylcarbonoimidoyl)carbamate 
• 152120-61-1 tert-butyl (amino(1H-pyrazol-1-yl)methylene)carbamate 
• 4023-02-3 1H-pyrazole-1-carboximidamide hydrochloride 
• 4023-00-1 1H-Pyrazole-1-carboxamidine 
• 313983-06-1 tert-butyl tert-butoxycarbonyl(((tert-butoxycarbonyl)imino)(1H-pyrazol-1-yl)methyl)carbamate 

Downstream Products

• 158478-70-7 N,N′-bis(tert-butoxycarbonyl)-N′′-cyclohexylguanidine 
• 158478-72-9 N,N′-bis(tert-butoxycarbonyl)-N′′-(4-methoxyphenyl)guanidine 
• 152120-58-6 N,N′-bis(tert-butoxycarbonyl)-N′′-(4-nitrophenyl)guanidine 
• 158478-76-3 (N,N'-bis(tert-butoxycarbonyl)carbamimidoyl)glycine 
• 41651-87-0 p-guanidinomethyl benzoic acid 
• 357339-51-6 C₃₇H₅₃N₅O₈ 
• 474801-75-7 C₃₅H₅₀N₄O₁₃ 
• 474801-73-5 C₃₄H₅₄N₄O₁₃ 
• 312760-49-9 C₃₅H₄₅N₅O₉S₂ 
• 312760-41-1 C₃₅H₄₅N₅O₉S₂ 
• 312760-45-5 C₃₅H₄₅N₅O₉S₂ 
• 312760-16-0 C₃₆H₄₇N₅O₉S₂ 
• 312760-27-3 C₃₉H₅₃N₅O₉S₂ 
• 312760-23-9 C₃₆H₄₇N₅O₉S₂ 

Relevant academic research and scientific papers

Synthesis and characterization of 4(R)-epimer impurities of zanamivir and laninamivir octanoate

The synthesis and characterization of compounds 7c and 8d, the 4(R)-epimer impurities of zanamivir and laninamivir octanoate, were reported for the first time. Their structures were confirmed by NMR and MS and distinguished from their corresponding active pharmaceutical ingredient (API) by coupling constant in 1H NMR and HPLC spectra. This work is of great significance for the drug-related substances analysis in zanamivir and laninamivir octanoate.

Hitting a Moving Target: Simulation and Crystallography Study of ATAD2 Bromodomain Blockers

Small molecule ligand binding to the ATAD2 bromodomain is investigated here through the synergistic combination of molecular dynamics and protein crystallography. A previously unexplored conformation of the binding pocket upon rearrangement of the gatekeeper residue Ile1074 has been found. Further, our investigations reveal how minor structural differences in the ligands result in binding with different plasticity of the ZA loop for this difficult-to-drug bromodomain.

RADIOIODINATED COMPOUNDS

This disclosure relates to reagents and methods useful in the synthesis of aryl iodines, for example, in the preparation of iodine labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.

PYRROLOPYRIMIDINE AND PURINE DERIVATIVES

The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

Structure-activity relationship study on α1 adrenergic receptor antagonists from beer

Hordatine A and aperidine have been previously isolated from beer as active ingredients, which bind to muscarinic M3 receptor. In addition, these compounds have exhibited antagonist activity against the α1A adrenoceptor. Although the relative structures of these two molecules have previously been determined, the absolute stereochemistry was unclear. Hence, to elucidate the absolute stereochemistry of natural hordatine A, we synthesized each enantiomer of hordatine A and aperidine from optically pure dehydrodi-p-coumaric acid. Several additional related compounds were also synthesized for structure-activity relationship studies. Chiral column HPLC analysis demonstrated that the absolute stereochemistry of natural hordatine A is (2S,3S), while based on the isomerization mechanism, the stereochemistry of aperidine is (2R,3S). The α1A adrenoceptor binding activity of (2R,3R)-hordatine A is the most potent among the enantiomeric pairs of hordatines and aperidines. Furthermore, the related, synthetic compound, (2R,3R)-methyl benzofurancarboxylate exhibits antagonist activity against the α1A adrenoceptor at a lower concentration than that of hordatine A.

METHOD FOR MANUFACTURING NEURAMINIC ACID DERIVATIVES

A method for manufacturing neuraminic acid derivatives is provided, also synthetic intermediates of the neuraminic acid derivatives and methods for their manufacture, and neuraminic acid derivatives having high purity. [Means for solution] A synthetic intermediate compound represented by the formula (7) is provided: [wherein R3 represents alkyl; R4 and R5 each represents H, alkyl, phenyl, or together represent tetramethylene, pentamethylene, oxo].

Non-peptide GnRH agents, methods and intermediates for their preparation

Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Optimisation of the synthesis of guanidines from amines via nitroguanidines using 3,5-dimethyl-N-nitro-1H-pyrazole-1-carboxamidine

The synthesis of the useful reagent for the preparation of guanidines, 3,5-dimethyl-N-nitro-1-pyrazole-1-carboxamidine (DMNPC), has been optimised. A detailed protocol for using this reagent for the preparation in pure form of a range of guanidines via nitroguanidines is described. A comparison has been made regarding efficiency between DMNPC and the guanidinylating reagents N,N′-bis-Boc-1-pyrazole-1-carboxamidine (2) and N,N′-bis-Boc- N′-triflylguanidine (3).

Non-peptide GnRH agents

Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and are defined variables: Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Transfection particles

Transfection particles for delivery of nucleic acid into higher eucaryotic cells in vitroand in vivocomprises one or more nucleic acid molecules condensed by organic cationic molecules. The discrete and stable particles are obtained by complexing the nucleic acid molecules with identical or different organic cationic precursor molecules without crosslinking nucleic acid molecules, and covalently linking the precursor molecules to each other on the nucleic acid template. For specific cellular targeting, the particles may carry targeting molecules, e.g. sugars. Preferred cationic precursor molecules are lipophilic detergents that are linked to form lipids. The particles contain preferably only one nucleic acid molecule which makes them useful for gene therapy and for delivery of large DNA molecules.