20263-26-7

Upstream product

• 65291-30-7 (R)-(+)-trityl glycidyl ether 
• 108-22-5 Isopropenyl acetate 
• 71697-18-2 1,2-propyleneglycol-1-triphenylmethyl ether 
• 138407-35-9 (R)-1-triphenylmethyloxy-2-acetoxypropane 
• 76-83-5 trityl chloride 
• 4254-14-2 (2R)-propane-1,2-diol 

Downstream Products

• 107148-84-5 (2R)-(-)-1-(triphenylmethoxy)-2-<(methylsulfonyl)oxy>propane 
• 179030-43-4 (R)-2-(dodecyloxy)-1-O-(triphenylmethyl)propane 
• 4254-14-2 (2R)-propane-1,2-diol 
• 210360-66-0 (R,R)-bis(1-methyl-2-triphenylmethyloxy)ethyl ether 
• 1259531-39-9 diisopropyl (R)-[(2-triphenylmethoxy-1-methylethyloxy)-methyl]phosphonate 
• 1443983-95-6 (R)-3-(fluoromethyl)-1-((S)-1-(trityloxy)propan-2-yl)pyrrolidine 
• 1443992-94-6 (R)-3-methoxy-1-((S)-1-(trityloxy)propan-2-yl)pyrrolidine 

Relevant academic research and scientific papers

Maximizing ER-α Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927

The further optimization of ER-α degradation efficacy of a series of ER modulators by refining side-chain substitution led to efficacious selective estrogen receptor degraders (SERDs). A fluoromethyl azetidine group was found to be preferred and resulted

DERIVATIVES OF 2,3-DIPHENYLCHROMENE USEFUL FOR THE TREATMENT OF CANCER

Described herein are compounds that are estrogen receptor modulators of Formula I and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. 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 c

ACYCLIC NUCLEOSIDE PHOSPHONATE DERIVATIVES AND MEDICINE USES THEREOF

An acyclic nucleoside phosphonate derivative and medicine use thereof are provided. In detail, an acyclic nucleoside phosphonate derivative shown in formula I is provided, which has potent antiviral activity (such as hepatitis B virus activity) and less cytotoxicity, and pharmaceutically-acceptable salts, isomers, hydrates or solvates thereof, where, R1 is selected from H or methyl; each R2 is independently selected from -R3 or -OR3; and each R3 is independently selected from C1-C8 alkyl or C3-C8 cycloalkyl. A preparation method of the compounds shown in formula I, a pharmaceutical composition containing the compounds, and a medical application thereof are also provided. The acyclic nucleoside phosphonate derivative is effective for antivirus, such as hepatitis B virus, and is good in vivo behavior attributes.

Resolution of a racemic 1,2-diol using triphenylmethyl protection of the primary hydroxyl group and Mucor miehei lipase (Lipozyme) for the kinetic resolution

The triphenylmethyl group gives very simple access to the 1-protection of 1,2-diol as exemplified by racemic propane-1,2-diol. This group has, however, been shown to be incompatible with lipases commonly used for the resolution of alcohols. This turned out to be the case for Pseudomonas cepacia lipase, which we have used in our earlier work. Lipozyme, a Mucor miehei lipase, best known for 1,3-selectivity with glycerol is, however, shown to catalyze transacetylation onto the secondary hydroxyl group next to a triphenylmethoxy group. The transacetylation is completely enantioselective for the (R)-enantiomer giving a very simple method for the resolution of this type of 1,2-diol enantiomer.

PYRIMIDINE SULPHONAMIDE DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.

Aminocyclopentadienyl Ruthenium Complexes as Racemization Catalysts for Dynamic Kinetic Resolution of Secondary Alcohols at Ambient Temperature

Aminocyclopentadienyl ruthenium complexes, which can be used as room-temperature racemization catalysts with lipases in the dynamic kinetic resolution (DKR) of secondary alcohols, were synthesized from cyclopenta-2,4-dienimines, Ru3(CO)12, and CHCl 3: [2,3,4,5-Ph4(η5-C 4CNHR)]Ru-(CO)2Cl (4: R = i-Pr; 5: R = n-Pr; 6: R = t-Bu), [2,5-Me2-3,4-Ph2(η5-C 4CNHR)]Ru(CO)2Cl (7: R = i-Pr; 8: R = Ph), and [2,3,4,5-Ph4(η5-C4CNHAr)]Ru(CO) 2Cl (9: Ar =p-NO2C6H4; 10: Ar = p-ClC6H4; 11: Ar = Ph; 12: Ar = p-OMeC6H 4; 13: Ar = p-NMe2C6H4). The tests in the racemization of (S)-4-phenyl-2-butanol showed that 7 is the most active catalyst, although the difference decreased in the DKR. Complex 4 was used in the DKR of various alcohols; at room temperature, not only simple alcohols but also functionalized ones such as allylic alcohols, alkynyl alcohols, diols, hydroxyl esters, and chlorohydrins were successfully transformed to chiral acetates. In mechanistic studies for the catalytic racemization, ruthenium hydride 14 appeared to be a key species. It was the major organometallic species in the racemization of (S)-1-phenylethanol with 4 and potassium tert-butoxide. In a separate experiment, (S)-1-phenylethanol was racemized catalytically by 14 in the presence of acetophenone.

Synthesis, biodistribution, and primate imaging of fluorine-18 labeled 2β-carbo-1'-fluoro-2-propoxy-3β-(4-chlorophenyl)tropanes. Ligands for the imaging of dopamine transporters by positron emission tomography

2β-(R)-Carbo-1-fluoro-2-propoxy-3β-(4-chlorophenyl)tropane ((R)-FIPCT, R-6) and 2β-(S)-carbo-1-fluoro-2-propoxy-3β-(4-chlorophenyl)tropane ((S)- FIPCT, S-6) were prepared and evaluated in vitro and in vivo for dopamine transporter (DAT) selectivity and sp

Improved Synthesis of (-)-(2R,6R)-2,6-Dimethylmorpholine

An improved procedure for obtaining the enantiomerically pure title amine is described, using a convergent synthesis, starting from the easily available (R)- and (S)-1,2-propanediols.