403705-10-2

Upstream product

• 27784-76-5 tert-butyl diethylphosphonoacetate 
• 15164-44-0 p-(iodophenyl)carboxaldehyde 
• 1663-39-4 tert-Butyl acrylate 
• 5122-99-6 4-iodophenylboronic acid 
• 86302-43-4 (tert-Butoxycarbonylmethylene)triphenylphosphorane 
• 13116-27-3 4-iodophenylhydrazine 
• 624-38-4 para-diiodobenzene 

Downstream Products

• 371919-40-3 tert-butyl (E)-3-(4-(diethoxyphosphoryldifluoromethyl)phenyl)prop-2-enoate 

Relevant academic research and scientific papers

Synthesis of a selective estrogen receptor degrader via a stereospecific elimination approach

An efficient synthesis of a selective estrogen receptor degrader, GDC-0810, bearing a challenging stereodefined (E)-tetrasubstituted all-carbon olefin core, is reported. The described synthetic route involves a highly diastereoselective addition of an ary

TARGETED PROTEIN DEGRADATION

This invention provides pharmaceutical protein degraders and E3 ubiquitin ligase binders for therapeutic applications as described further herein.

Improving reactivity and selectivity of aqueous-based Heck reactions by the local hydrophobicity of phosphine ligands

Modification of a triarylphosphine with a cholate moiety affords a new ligand, 1, which is effective in palladium-catalyzed Heck cross-couplings between acrylates and aryl iodides under mild, aqueous reaction conditions. High yields, up to 99%, were achieved in water at 40 °C. In competition studies, a more hydrophobic substrate (n-Bu acrylate) was preferred over the least hydrophobic substrate (methyl acrylate), supportive of a localized hydrophobic microenvironment near the catalytic center. The enhanced reactivity and selectivity for hydrophobic substrates disappeared when the local hydrophobicity was eliminated using a standard water-soluble phosphine or in organic solvents.

POLYCYCLIC ESTROGEN RECEPTOR MODULATORS AND USES THEREOF

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

ESTROGEN RECEPTOR MODULATORS AND USES THEREOF

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Synthesis and ring openings of cinnamate-derived N-unfunctionalised aziridines

Tert-Butyl cinnamates are aziridinated with high trans-selectivity by an N-N ylide generated in situ from N-methylmorpholine and O-diphenylphosphinyl hydroxylamine. The resulting N-unfunctionalised aziridines are shown to be versatile synthetic building b

Palladium-catalyzed C-C bond formation of arylhydrazines with olefins via carbon-nitrogen bond cleavage

The unactivated carbon-nitrogen bond of various aryl hydrazines was cleaved under very mild conditions by Pd(0) with the assistance of Pd(II). The in situ generated aryl palladium complex readily takes part in the C-C bond formation with olefins. This study offered a new mode of C-Pd bond formation, which will spur the development of palladium-catalyzed cross-coupling in the future.

Synthesis of phosphatase-stable, cell-permeable peptidomimetic prodrugs that target the SH2 domain of Stat3

The synthesis of prodrugs targeted to the SH2 domain of Stat3 is reported. Using a convergent strategy, the pivaloyloxymethyl phosphonodiester of pentachlorophenyl 4-phosphonodifluoromethylcinnamate, a phosphotyrosine surrogate, was synthesized and used t

Chemoselective three-component coupling via a tandem Pd-catalyzed boron-Heck and Suzuki reactions

A new approach is herein reported to prepare biaryl derivatives via a tandem Pd-catalyzed boron-Heck and Suzuki reactions. This one-pot tandem process avoided purification or addition of extra catalyst between steps. The resulting biaryl compounds can be

Inhibitors of signal transduction and activator of transcription 3

Stat3 inhibitor compounds are disclosed, wherein the compounds are structural analogs of Ac-pTyr-Leu-Pro-Gln-Thr-NH2 and bind to the SH2 domain of Stat3 under physiological conditions to inhibit a cellular signaling activity of Stat3.