620627-27-2

Basic information

• Product Name: 1-Pyrrolidineethanol,beta,3-dimethyl-,(betaS,3R)-(9CI)
• Synonyms: 1-Pyrrolidineethanol,beta,3-dimethyl-,(betaS,3R)-(9CI)
• CAS NO: 620627-27-2
• Molecular Formula: C₈H₁₇NO
• Molecular Weight: 143.23
• Product Categories: AMINETERTIARY
• Mol File: 620627-27-2.mol
• Article Data: 8

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 1-Pyrrolidineethanol,beta,3-dimethyl-,(betaS,3R)-(9CI)(CAS DataBase Reference)
• NIST Chemistry Reference: 1-Pyrrolidineethanol,beta,3-dimethyl-,(betaS,3R)-(9CI)(620627-27-2)
• EPA Substance Registry System: 1-Pyrrolidineethanol,beta,3-dimethyl-,(betaS,3R)-(9CI)(620627-27-2)

Safety Data

• Hazardous Substances Data: 620627-27-2(Hazardous Substances Data)

Upstream product

• 2938-98-9 (R)-2-methylbutane-1,4-diol 
• 22644-27-5 (R)-methylsuccinic acid dimethyl ester 
• 2749-11-3 (S)-Alaninol 
• 69498-28-8 (R)-1,4-dibromo-2-methylbutane 
• 2174-58-5 L-malic acid 
• 3641-51-8 2-(R)-methylsuccinic acid 
• 620627-28-3 (R)-1-((S)-2-Hydroxy-1-methyl-ethyl)-3-methyl-pyrrolidine-2,5-dione 

Downstream Products

• 620627-17-0 (R)-1-((S)-2-{4-[(2S,3R)-6-Benzyloxy-3-(3-triisopropylsilanyloxy-phenyl)-2,3-dihydro-benzo[1,4]oxathiin-2-yl]-phenoxy}-1-methyl-ethyl)-3-methyl-pyrrolidine 
• 1352547-08-0 (3R)-1-((2S)-1-(4-(5-methoxy-2-(4-methoxyphenyl)-2,3-dihydro-1H-inden-1-yl)phenoxy)propan-2-yl)-3-methylpyrrolidine 
• 1352546-95-2 2-(4-hydroxyphenyl)-1-(4-((S)-2-((R)-3-methylpyrrolidin-1-yl)propoxy)phenyl)-2,3-dihydro-1H-inden-5-ol 
• 1352547-09-1 2,3-bis(3-methoxyphenyl)-1-(4-((S)-2-((R)-3-methylpyrrolidin-1-yl)propoxy)phenyl)propan-1-one 
• 1352547-07-9 (R)-1-((S)-1-(4-(6-methoxy-2-(4-methoxyphenyl)-1H-inden-3-yl)phenoxy)propan-2-yl)-3-methylpyrrolidine 
• 1352308-01-0 3-(4-fluorophenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-1-yl)propoxy)phenyl)-2H-chromen-6-ol 
• 1352307-45-9 3-(3-fluorophenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-1-yl)propoxy)phenyl)-2H-chromen-6-ol hydrochloride 
• 1352307-40-4 4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-1-yl)propoxy)phenyl)-3-phenyl-2H-chromen-6-ol hydrochloride 
• 1352307-39-1 3-(4-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-1-yl)propoxy)phenyl)-2H-chromen-7-ol trifluoroacetate 
• 1352307-44-8 3-(4-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-1-yl)propoxy)phenyl)-2H-chromen-6-ol hydrochloride 
• 1352307-37-9 3-(3-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-1-yl)propoxy)phenyl)-2H-chromen-7-ol trifluoroacetate 
• 1352306-69-4 (R)-3-(3-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-1-yl)propoxy)phenyl)-2H-chromen-6-ol 
• 1352306-67-2 (S)-3-(3-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-1-yl)propoxy)phenyl)-2H-chromen-6-ol 

Relevant articles and documents

Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer

About 75% of breast cancers are estrogen receptor alpha (ER-α) positive, and women typically initially respond well to antihormonal therapies such as tamoxifen and aromatase inhibitors, but resistance often emerges. Fulvestrant is a steroid-based, selective estrogen receptor degrader (SERD) that both antagonizes and degrades ER-α and shows some activity in patients who have progressed on antihormonal agents. However, fulvestrant must be administered by intramuscular injections that limit its efficacy. We describe the optimization of ER-α degradation efficacy of a chromene series of ER modulators resulting in highly potent and efficacious SERDs such as 14n. When examined in a xenograft model of tamoxifen-resistant breast cancer, 14n (ER-α degradation efficacy = 91%) demonstrated robust activity, while, despite superior oral exposure, 15g (ER-α degradation efficacy = 82%) was essentially inactive. This result suggests that optimizing ER-α degradation efficacy in the MCF-7 cell line leads to compounds with robust effects in models of tamoxifen-resistant breast cancer derived from an MCF-7 background.

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INDANE 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.