1143572-00-2

Usage

Uses

Used in Organic Synthesis:
(Z)-tert-butyl (((tert-butoxycarbonyl)imino)(1H-pyrazol-1-yl)methyl)carbamate is used as a reagent in organic synthesis for its ability to facilitate the formation of complex molecular structures. Its unique functional groups contribute to its versatility in creating a wide range of chemical products.
Used in Pharmaceutical Research:
In the pharmaceutical industry, (Z)-tert-butyl (((tert-butoxycarbonyl)imino)(1H-pyrazol-1-yl)methyl)carbamate is used as a key intermediate in the development of new drugs. Its structural properties make it a promising candidate for the creation of bioactive molecules with potential therapeutic applications.
Used in Drug Development:
(Z)-tert-butyl (((tert-butoxycarbonyl)imino)(1H-pyrazol-1-yl)methyl)carbamate is utilized in drug development due to its potential to be incorporated into novel pharmaceutical compounds. Its functional groups and reactivity allow for the design and synthesis of molecules with specific biological activities, targeting various medical conditions.

Upstream product

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

Downstream Products

• 158478-72-9 N,N′-bis(tert-butoxycarbonyl)-N′′-(4-methoxyphenyl)guanidine 
• 158478-76-3 (N,N'-bis(tert-butoxycarbonyl)carbamimidoyl)glycine 
• 145315-38-4 H-L-Arg(Boc)₂-OH 
• 41651-87-0 p-guanidinomethyl benzoic acid 
• 83585-01-7 Cbz-Arg(Boc)2-OH 
• 333406-04-5 (5S)-5-[(2S)-2-benzyloxycarbonylamino-3-(trityl-carbamoyl)-propionylamino]-(4S)-4-(tert-butyl-dimethyl-silanyloxy)-(2R)-2-(3-N,N'-bis-t-boc-guanidino-propyl)-6-phenyl-hexanoic 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 

Relevant academic research and scientific papers

A convenient preparation of monosubstituted N,N'-di(Boc)-protected guanidines

1-H-Pyrazole-1-[N,N'-bis(tert-butoxycarbonyl)]carboxamidine (1) reacts under mild conditions with a number of amines and amino acids to give the respective protected guanidines in moderate to high isolated yields.

An efficient method for the preparation of ω,ω'-bis-urethane protected arginine derivatives

Fmoc-Arg(ω,w')(Boc)2-OH and Boc-Arg(ω,w')(Cbz)2-OH were prepared in two steps: Guanylation of Cu(II)-ornithine complex at N(δ) with N,N'-bis urethane protected derivatives of 1-guanylpyrazole, followed by N(α)-protection using either 9-fluorenylmethyl succinimidylcarbonate or di-t-butyl-dicarbonate in the presence of EDTA. The overall yields of these products (2 steps) were 65% and 73%.

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).

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.