Antioxidant BHT 264
CAS:128-37-0
Purity:99%
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Relugolix is a highly selective, oral, nonpeptide GnRH antagonist being investigated as a possible prostate cancer treatment
2,6-difluorobenzyl chloride
TAK-385
| Conditions | Yield |
|---|---|
|
Multi-step reaction with 7 steps
1.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 5 h / 100 °C
2.1: potassium carbonate / 3 h / 60 °C
3.1: tetrahydrofuran / 5 h / 70 °C
4.1: N-Bromosuccinimide; 2,2'-azobis(isobutyronitrile) / tetrachloromethane / 4 h / Reflux
5.1: potassium carbonate / N,N-dimethyl-formamide / 5 h / 80 °C
6.1: hydrogen; palladium 10% on activated carbon / ethanol / 6 h / 20 °C
7.1: N-ethyl-N,N-diisopropylamine / acetonitrile / 0.5 h / 20 °C
7.2: 4.5 h / 50 °C
With
N-Bromosuccinimide; 2,2'-azobis(isobutyronitrile); palladium 10% on activated carbon; hydrogen; potassium carbonate; N-ethyl-N,N-diisopropylamine;
In
tetrahydrofuran; tetrachloromethane; ethanol; N,N-dimethyl-formamide; acetonitrile;
|
C31H33F2N7O6S
TAK-385
| Conditions | Yield |
|---|---|
|
With
1,8-diazabicyclo[5.4.0]undec-7-ene;
In
methanol;
at 0 ℃;
|
89% |
|
With
sodium methylate;
In
methanol;
at 30 - 40 ℃;
for 1h;
|
86.3% |
|
With
sodium methylate;
In
methanol; N,N-dimethyl acetamide;
at 60 ℃;
for 6h;
Reagent/catalyst;
|
84.9% |
The CAS number of TAK-385 is 737789-87-6.
More information of TAK-385 737789-87-6 are:
|
CAS Number |
737789-87-6 |
|
Density |
1.442±0.06 g/cm3(Predicted) |
|
Melting Point |
228 °C (decomp)(Solv: ethyl acetate (141-78-6); tetrahydrofuran (109-99-9)) |
|
PSA |
182.86000 |
|
LogP |
3.69890 |
|
Pka |
13.17±0.70(Predicted) |
Synonyms for TAK-385 737789-87-6:1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea;TAK-385;
The chemical formula of TAK-385 is C29H27F2N7O5S which containing 29 Carbon atoms,27 Hydrogen atoms,2 Fluorine atoms,7 Nitrogen atoms,5 Oxygen atoms and 1 Sulfur atoms,and the molecular weight of TAK-385 is 623.63.
Relugolix (TAK-385)?is a potent, orally active, nonpeptidic?gonadotropin-releasing hormone (GnRH)?antagonist. It possesses high affinity and potent antagonistic activity for human receptor (binding?IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209). Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al.
Relevant articles related to TAK-385:
|
Article |
Source |
|
Preparation method of Rurugolix |
- , (2022/03/31) |
|
Preparation method of Relugolix |
- Paragraph 0103-0107, (2021/10/16) |
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