Day: October 26, 2022

Li, Yitao; Yao, Wenqiang; Lin, Jian; Li, Falin; Wu, Yang; Xu, Junxing published an article in 2019, the title of the article was Design, Synthesis and Biological Activity of Novel Triazole Sulfonamide Derivatives Containing a Benzylamine Moiety.Synthetic Route of 16296-68-7 And the article contains the following content:

The 1,2,4-triazole-1,3-disulfonamide derivatives I [Ar = 2-thienyl, 2-pyrrolyl, 3-pyridyl, etc.] were synthesized via coupling of amines with triazole sulfonamide groups and evaluated for their fungicidal activity against cucumber downy mildew (CDM). Most of these derivatives exhibited better fungicidal activities than that of the com. cyanosole using bioassays. In particular, compounds I [Ar = 4-bromo-2-thiazolyl, 5-chloro-2-thienyl] showed the best fungicidal activity against CDM (EC50 = 6.91 and 10.62 mg/L). Comparative experiments demonstrated that the fungicidal activity of I [Ar = 4-bromo-2-thiazolyl, 5-chloro-2-thienyl] was better than the com. pesticides amisulbrom and cyanosole. The experimental process involved the reaction of 5-Chlorobenzo[b]thiophene-3-carbaldehyde(cas: 16296-68-7).Synthetic Route of 16296-68-7

The Article related to triazole disulfonamide benzylamine preparation fungicidal, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Synthetic Route of 16296-68-7

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

On March 21, 1997, Taylor, Edward C.; Dowling, James E. published an article.Safety of 3-Bromo-4,5,6,7-tetrahydrobenzo[c]thiophene-1-carboxylic acid The title of the article was Replacement of the 1′,4′-Phenylene Region in 5,10-Dideaza-5,6,7,8-tetrahydrofolic Acid (DDATHF) by 4,5,6,7-Tetrahydrobenzo[c]thiophene and 4,5,6,7-Tetrahydroisobenzofuran Nuclei. And the article contained the following:

Two new analogs of DDATHF, in which the 1′,4′-phenylene unit is replaced by 4,5,6,7-tetrahydrobenzo[c]thiophene and 4,5,6,7-tetrahydroisobenzofuran nuclei, have been prepared and evaluated for in vitro cytotoxicity, glycinamide ribonucleotide formyltransferase (GARFT) inhibition, and folyl polyglutamate synthetase (FPGS) affinity as potential antitumor agents. The experimental process involved the reaction of 3-Bromo-4,5,6,7-tetrahydrobenzo[c]thiophene-1-carboxylic acid(cas: 188240-63-3).Safety of 3-Bromo-4,5,6,7-tetrahydrobenzo[c]thiophene-1-carboxylic acid

The Article related to dideazatetrahydrofolate derivative preparation antitumor, glycinamide ribonucleotide formyltransferase inhibition dideazatetrahydrofolate derivative, folyl polyglutamate synthetase affinity dideazatetrahydrofolate derivative and other aspects.Safety of 3-Bromo-4,5,6,7-tetrahydrobenzo[c]thiophene-1-carboxylic acid

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

On January 28, 2021, Cuthbertson, Alan; Boehnke, Niels published a patent.Formula: C9H5ClOS The title of the patent was Targeted radiopharmaceuticals for the diagnosis and treatment of prostate cancer. And the patent contained the following:

The invention is related to the preparation of compounds I [n = 1-3; R1-4 = OH or Q; Q = a tissue-targeting moiety selected from the group consisting of poly- and oligopeptides, proteins, DNA and RNA fragments, aptamers polyclonal or monoclonal antibodies, and a mixture of proteins or fragments or constructs of protein] their stereoisomers, hydrates, solvates and salts, and targeted radiopharmaceuticals, pharmaceutical compositions and combinations comprising them and their use for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of soft tissue diseases, as a sole agent or in combination with other active ingredients. The experimental process involved the reaction of 5-Chlorobenzo[b]thiophene-3-carbaldehyde(cas: 16296-68-7).Formula: C9H5ClOS

The Article related to peptide chelator conjugate preparation antitumor prostate cancer, preparation peptide chelator thorium 227 her2 fap psma conjugate, prostate specific membrane antigen carboxy hopo thorium 227 conjugate, targeted radiopharmaceutical prostate cancer and other aspects.Formula: C9H5ClOS

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

On May 8, 2019, Kurz, Guido; Camacho Gomez, Juan published a patent.Application In Synthesis of 5-Chlorobenzo[b]thiophene-3-carbaldehyde The title of the patent was Preparation of novel dihydropyridine derivatives as androgen receptor and glucocorticoid receptor modulators. And the patent contained the following:

The present invention relates to novel dihydropyridine derivatives I [R1 = CN, CHO, COR5, CO2R5 (wherein R5 = (un)substituted alkyl, cycloalkyl); R2 = CN, COR8, CO2R8, SOnR8, C(O)NR8R9 (n = 1-2; R8 and R9 = (independently) H, (un)substituted alkyl, cycloalkyl, etc.; or R8 and R9 together with the nitrogen atom to which they are attached form (un)substituted 5-6 membered heterocycle which optionally comprises 1 heteroatom selected from O and N); R3 = H, NH2, CN, etc.; R4 = H, CN, (un)substituted alkyl, etc.; or R1 and R3 or R2 and R4 form together (CR10R11)n (n = 3-4 wherein 1, 2 or 3 of CR10R11 moieties may be independently replaced by a group selected from O, S, C(O) and (un)substituted NH; R10, R11 = (independently) H, (un)substituted Ph or 5-6 membered heteroaryl, etc.); X1-X5 = (independently) CB1, N and CH (B1 = halo, CN, (un)substituted 5-6 membered heteroaryl, etc.)] and pharmaceutically acceptable salts thereof, as modulators of nuclear receptors selected from androgen receptor and glucocorticoid receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said for manufacturing a medicament for the treatment of pathol. conditions or diseases that can improve by modulation of androgen receptor and/or glucocorticoid receptor, selected from cancer, metastasizing cancers, benign prostate hyperplasia, polycystic ovary syndrome (PCOS), hair loss, hirsutism, acne, hypogonadism, muscle wasting diseases, cachexia, Cushing’s syndrome, anti-psychotic drug induced weight gain, obesity, post-traumatic stress disorder and alcoholism. Over two-hundred-seventy compounds I were prepared For example, heating a mixture of 3-(benzo[b]thiophen-3-ylmethylene)pentane-2,4-dione, Me 3-oxobutanoate and 30% aqueous ammonium in iso-PrOH at reflux temperature for 12 h afforded 25% II (both enantiomers were separated). Exemplified compounds I were evaluated for their androgen receptor and glucocorticoid receptor modulatory activities (data given for representative compounds I). The experimental process involved the reaction of 5-Chlorobenzo[b]thiophene-3-carbaldehyde(cas: 16296-68-7).Application In Synthesis of 5-Chlorobenzo[b]thiophene-3-carbaldehyde

The Article related to pyridine dihydropyridine preparation nuclear androgen glucocorticoid receptor modulator antitumor, benign prostate hyperplasia polycystic ovary syndrome treatment dihydropyridine preparation, hair loss hirsutism acne hypogonadism treatment dihydropyridine pyridine preparation and other aspects.Application In Synthesis of 5-Chlorobenzo[b]thiophene-3-carbaldehyde

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

On May 9, 2019, Kurz, Guido; Camacho Gomez, Juan published a patent.Synthetic Route of 16296-68-7 The title of the patent was Preparation of novel dihydropyridine derivatives as androgen receptor and glucocorticoid receptor modulators. And the patent contained the following:

The present invention relates to novel dihydropyridine derivatives I [R1 = CN, C(O)NH2, COR5, CO2R5 (wherein R5 = (un)substituted alkyl, cycloalkyl); R2 = CN, COR8, CO2R8, SOnR8, C(O)NR8R9 (n = 1-2; R8 and R9 = (independently) H, (un)substituted alkyl, H, etc.; or R8 and R9 together with the nitrogen atom to which they are attached form (un)substituted 5-6 membered heterocycle which optionally comprises 1 heteroatom selected from O and N); R3 = H, NH2, CN, etc.; R4 = H, CN, (un)substituted alkyl, etc.; X1-X5 = (independently) CB1, N and CH (B1 = halo, CN, (un)substituted 5-6 membered heteroaryl, etc.)] and pharmaceutically acceptable salts thereof, as modulators of nuclear receptors selected from androgen receptor and glucocorticoid receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said for manufacturing a medicament for the treatment of pathol. conditions or diseases that can improve by modulation of androgen receptor and/or glucocorticoid receptor, selected from cancer, metastasizing cancers, benign prostate hyperplasia, polycystic ovary syndrome (PCOS), hair loss, hirsutism, acne, hypogonadism, muscle wasting diseases, cachexia, Cushing’s syndrome, anti-psychotic drug induced weight gain, obesity, post-traumatic stress disorder and alcoholism. Over three-hundred compounds I were prepared For example, heating a mixture of 3-(benzo[b]thiophen-3-ylmethylene)pentane-2,4-dione, Me 3-oxobutanoate and 30% aqueous ammonium in iso-PrOH at reflux temperature for 12 h afforded 25% II (both enantiomers were separated). Exemplified compounds I were evaluated for their androgen receptor and glucocorticoid receptor modulatory activities (data given for representative compounds I). The experimental process involved the reaction of 5-Chlorobenzo[b]thiophene-3-carbaldehyde(cas: 16296-68-7).Synthetic Route of 16296-68-7

The Article related to pyridine dihydropyridine preparation nuclear androgen glucocorticoid receptor modulator antitumor, benign prostate hyperplasia polycystic ovary syndrome treatment dihydropyridine preparation, hair loss hirsutism acne hypogonadism treatment dihydropyridine pyridine preparation and other aspects.Synthetic Route of 16296-68-7

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem