51458-31-2

Upstream product

• 501-97-3 4-hydroxyphenylpropionic acid 
• 75-65-0 tert-butyl alcohol 
• 691905-29-0 tert-butyl (E)-3-(4-benzyloxyphenyl)propenoate 
• 530-62-1 1,1'-carbonyldiimidazole 
• 1694-31-1 tert-butyl acetoacetate 
• 106-41-2 4-bromo-phenol 
• 1663-39-4 tert-Butyl acrylate 
• 540-38-5 p-Iodophenol 

Downstream Products

• 1160755-29-2 3-(4-methoxycarbonylmethoxyphenyl)propionic acid tert-butyl ester 
• 114643-30-0 4-hydroxy-trans-cinnamic acid tert-butyl ester 

Relevant academic research and scientific papers

A Convenient Synthesis for HBED-CC-tris(tert -butyl ester)

HBED-CC is a bifunctional complexing agent that, at ambient temperature, tightly chelates the trivalent radiometal 68 Ga (T 1/2 = 68 min). This complexing agent has attracted a lot of interest in tumor imaging applications. Depending on the chemical structure, different HBED-CC variants may be employed as radiolabeling precursor for the synthesis of desired radiopharmaceuticals. In this context, HBED-CC-tris(tert-butyl ester) is the only known monovalent variant of HBED-CC which is used for the synthesis of non-symmetric HBED-CC-based radiopharmaceuticals. Commercial HBED-CC-tris(tert -butyl ester) is very expensive, with limited availability. Nevertheless, no synthetic procedure for this useful product has been reported to date. This work introduces a convenient and comparatively cost-efficient method for the preparation of HBED-CC-tris(tert -butyl ester).

Synthesis of HBED–CC–tris(tert-butyl ester) using a solid phase and a microwave reactor

N,N′-bis-[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N′-diacetic acid (HBED-CC) belongs to the acyclic, bifunctional complexing compounds used mainly for radiolabeling with gallium-68 (68Ga). Due to the high stability of the 68Ga3+complex, HBED-CC is well known for its rapid and efficient labeling at ambient temperature and the high stability of the complexes in vivo. The HBED-CC chelator in combination with a PSMA (Prostate Specific Membrane Antigen) inhibitor and labeled with isotope of gallium is an important tool for diagnosing the stage of cancer in patients with prostate cancer. Many HBED-CC derivatives have been described in the literature, but one of the most commonly used is 3-(3-{[(2-{[5-(2-tert-butoxycarbonylethyl)-2-hydroxybenzyl]-tert-butoxycarbonylmethylamino}-ethyl)-tert-butoxy-carbonylmethylamino]-methyl}-4-hydroxyphenyl)propionic acid (HBED–CC–tris(tert-butyl ester)). This compound is very expensive and commercially limited. Therefore this work describes an innovative method of synthesis on solid phase using of a microwave reactor. Optimization of the reaction allowed to obtain HBED-CC-tris(tert-butyl ester) with high purity and yield.

POLYMER PARTICLES

Described are polymers and methods of forming and using same.

Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases

The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.

Ti/Ni-mediated inter- and intramolecular conjugate addition of aryl and alkenyl halides and triflates

In this work, we show that the unique combination of a nickel catalyst and Cp2TiCl allows the direct conjugate addition of aryl and alkenyl iodides, bromides, and to a lesser extent, chlorides and triflates to α,β-unsaturated carbonyls at room temperature, without requiring the previous formation of an organometallic nucleophile. The reaction proceeds inter- and intramolecularly with good functional group compatibility, which is key for the development of free protecting group methodologies. Carbo- and heterocycles of five- and six-membered rings are obtained in good yields. Moreover, some insights about the mechanism involved have been obtained from cyclic voltammetry, UV-vis, and HRTEM measurements.

COMPOSITIONS FOR TREATMENT OF CYSTIC FIBROSIS AND OTHER CHRONIC DISEASES

The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.

Organic Compounds

A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Intracellular trapping of cyclosal-pronucleotides: Modification of prodrugs with amino acid esters

A new class of d4TMP-cycloSal-pronucleotides bearing enzymatically cleavable amino acid esters is reported. These compounds are designed to trap the pronucleotide inside the cell by a fast conversion of a nonpolar ester group into a charged carboxylate. This should prevent efficient diffusion equilibrium across the cell membrane to the extracellular environment, leading to an intracellular accumulation of the compounds. This initial conversion is followed by a slow release of the nucleoside monophosphate (i.e., d4TMP). The concept is proven by hydrolysis studies in phosphate buffer, cell extracts, and human serum. These investigations revealed a high sensitivity of some amino acid ester modifications to conversion by cellular extracts, resulting in the fast release of a charged intermediate, whereas no cleavage of the modification is found in phosphate buffer. In addition, antiviral activities against HIV are presented.

Indium(III) acetate-catalyzed intermolecular radical addition of organic iodides to electron-deficient alkenes

In the presence of phenylsilane and a catalytic amount of indium(III) acetate, organic iodides added to electron-deficient alkenes in ethanol at room temperature. Both simple and functionalized organic iodides were applicable to this reaction. A plausible reaction mechanism involves the formation of indium hydride species by hydride transfer from silicon to indium and an indium hydride-mediated radical chain process.

Pd-C-induced catalytic transfer hydrogenation with triethylsilane

(Chemical Equation Presented) In situ generation of molecular hydrogen by addition of triethylsilane to palladium-charcoal catalyst results in rapid and efficient reduction of multiple bonds, azides, imines, and nitro groups, as well as benzyl group and allyl group deprotection under mild, neutral conditions.