Category: 53788-12-8

On June 12, 1974, Jeanmart, Claude; Leger, Andre; Messer, Mayer N. published a patent.Recommanded Product: 4-Ethyl-piperazine-1-carbonyl chloride The title of the patent was [1,4]Dithiino[2,3-c]pyrrole derivatives. And the patent contained the following:

Dithiinopyrrolyl esters I (R =substituted 2-pyridyl, 2-naphthyridinyl, phenyl, 6-methoxy-3-pyridazinyl, 7-chloro-2-quinolyl, R1 = Me; R1 = Et, CHMe2, allyl, CH2CH2OH, R = 5-chloro-2-pyridyl) (25 compounds) were prepared by esterifying the alcs. II (R2 = OH, R3 = H), prepared by treating III with RNH2 and reducing II (R2R3 = O). Thus, 35. g III was treated with 24 g 2-amino-5-chloropyridine to give 51 g II (R = 5-chloro-2-pyridyl, R2R3 = O), which was reduced with KBH4 to 49.8 g II (R2 = OH, R3 = H). Esterification of 15 g of the alc. with 24.4 g 1-(chlorocarbonyl)-4-methylpiperazine gave 15.6 g I (R = 5-chloro-2-pyridyl, R1 = Me). I were tranquilizing, anticonvulsant, and muscle relaxant at 5-100 mg/kg orally in mice. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Recommanded Product: 4-Ethyl-piperazine-1-carbonyl chloride

The Article related to dithiinopyrrolyl ester, anticonvulsant dithiinopyrrolyl ester, muscle relaxant dithiinopyrrolyl ester, tranquilizer dithiinopyrrolyl ester, piperazine dithiinopyrrolyl ester and other aspects.Recommanded Product: 4-Ethyl-piperazine-1-carbonyl chloride

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On January 22, 1998, Shimizu, Hideaki; Abe, Atsuhiro; Yaegashi, Takashi; Sawada, Seigo; Nagata, Hiroshi published a patent.HPLC of Formula: 53788-12-8 The title of the patent was Preparation of taxane derivatives as antitumors and pharmaceuticals containing them. And the patent contained the following:

The title compounds [I; X, Y = CO-A-B; A = bond, -R-CO-, -R-OCO-, -R-NHCO-; R = alkylene, phenylene; B = (un)substituted heterocyclyl, e.g., piperazin-1-yl; Z = H, trialkylsilyl, trihaloalkoxycarbonyl; Bz = benzoyl], II [R7 = H, alkoxycarbonyl, aralkyloxycarbonyl; R8, R9 = H, alkyl, haloalkyl, etc.] or their salts are prepared Thus, 7-O-triethylsilyl-10-deacetylbaccatin III was reacted with 4-(dimethylamino)piperidinocarbonyl chloride (also prepared) in THF-hexane containing BuLi at -40° to room temperature to give 90% 10-O-(4-dimethylaminopiperidinocarbonyl)-7-O-triethylsilyl-10-deacetylbaccatin III. This was reacted with (4S,5R)-3-(benzyloxycarbonyl)-2,2-dimethyl-4-phenyl-5-oxazolidinecarboxylic acid to give the title compound III. These compounds exhibit a high solubility in water and showed excellent antitumor activity. In an ELISA screening using human oral cancer KB cells, the GI50 for 13-O-[3-(tert-butoxycarbonylamino)-2-hydroxy-3-phenylpropionyl]-10-O-(4-dipropylaminopiperidinocarbonyl)-10-deacetylbaccatin III (also prepared) was 0.78 ng/mL vs. 2.0 ng/mL for taxol. The solubility of 13-O-[3-(tert-butoxycarbonylamino)-2-hydroxy-3-phenylpropionyl]-10-O-(4-dimethylaminopiperidinocarbonyl)-10-O-deacetylbaccatin III (also prepared) in water was 1260 μg/mL vs. 0.4 μg/mL for taxol. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).HPLC of Formula: 53788-12-8

The Article related to taxane derivative preparation antitumor solubility, Terpenes and Terpenoids: Diterpenes (C20), Including Gibberellins, Retinoids, Quassinoids, and Tocopherols and other aspects.HPLC of Formula: 53788-12-8

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On August 1, 2012, Li, Qingeng; Wang, Tao; Xia, Biao; Guo, Bin published a patent.Category: piperazines The title of the patent was Novel 7,10-O,O-dimethyldocetaxel derivative, its preparation process and application for treating cancers. And the patent contained the following:

The invention disclosed a kind of 7,10-O,O-dimethyldocetaxel derivatives and their salts, preparation method and medical application as antitumor agents. The claimed title compounds are shown in structure I (R = H, Me, Et, Pr, iso-Pr, Bu, iso-Bu, or CH2-Ph; HB = inorganic or organic acid from HCl, HBr, HNO3, acetic acid, lactic acid, or tartaric acid etc.). The claimed compounds are prepared with II via esterification etc. multiple steps (procedure given). The obtained compounds and pharmaceutically acceptable salts can be used for preparing water-soluble medicals for treating cancers such as breast cancer, lung cancer and ovarian cancer without side effect, high safety and controlled quality (no data provided). The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Category: piperazines

The Article related to dimethyldocetaxel derivative salt synthesis esterification antitumor agent, Terpenes and Terpenoids: Diterpenes (C20), Including Gibberellins, Retinoids, Quassinoids, and Tocopherols and other aspects.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On August 24, 2016, Li, Qingshan; Zhang, Yuanlin; Feng, Xiue published a patent.Formula: C7H13ClN2O The title of the patent was Preparation of N-formyloxy substituted chlorobenzophenone derivatives. And the patent contained the following:

The invention discloses structure construction of N-formyloxy substituted chlorobenzophenone novel derivative I; in its structure R is N-formyl group; wherein two hydrogen atoms on nitrogen atom are substituted by two same straight-chain alkyls or branched alkyls with carbon atom of 1-4, or two hydrogen atoms on nitrogen atom are substituted to generate pyrrole ring, piperazine ring, piperidine ring, morpholine ring. Meanwhile, the invention discloses application of the N-formyloxy substituted chlorobenzophenone novel derivative and its pharmaceutical salts in preparing medicines for cardiovascular disease caused by vascular endothelial cell injury. The N-formyloxy substituted chlorobenzophenone derivative of the invention can remarkably improve protection activity to H2O2 induced vascular endothelial cell injury, and it has important application prospect in preparing related medicine for preventing or treating cardiovascular disease caused by vascular endothelial cell injury. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Formula: C7H13ClN2O

The Article related to preparation formyloxy substituted chlorobenzophenone derivative, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Ketones and Derivatives, Including Quinones and Sulfur Analogs and other aspects.Formula: C7H13ClN2O

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On June 12, 1974, Jeanmart, Claude; Leger, Andre; Messer, Mayer N. published a patent.Recommanded Product: 4-Ethyl-piperazine-1-carbonyl chloride The title of the patent was [1,4]Dithiino[2,3-c]pyrrole derivatives. And the patent contained the following:

Dithiinopyrrolyl esters I (R =substituted 2-pyridyl, 2-naphthyridinyl, phenyl, 6-methoxy-3-pyridazinyl, 7-chloro-2-quinolyl, R1 = Me; R1 = Et, CHMe2, allyl, CH2CH2OH, R = 5-chloro-2-pyridyl) (25 compounds) were prepared by esterifying the alcs. II (R2 = OH, R3 = H), prepared by treating III with RNH2 and reducing II (R2R3 = O). Thus, 35. g III was treated with 24 g 2-amino-5-chloropyridine to give 51 g II (R = 5-chloro-2-pyridyl, R2R3 = O), which was reduced with KBH4 to 49.8 g II (R2 = OH, R3 = H). Esterification of 15 g of the alc. with 24.4 g 1-(chlorocarbonyl)-4-methylpiperazine gave 15.6 g I (R = 5-chloro-2-pyridyl, R1 = Me). I were tranquilizing, anticonvulsant, and muscle relaxant at 5-100 mg/kg orally in mice. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Recommanded Product: 4-Ethyl-piperazine-1-carbonyl chloride

The Article related to dithiinopyrrolyl ester, anticonvulsant dithiinopyrrolyl ester, muscle relaxant dithiinopyrrolyl ester, tranquilizer dithiinopyrrolyl ester, piperazine dithiinopyrrolyl ester and other aspects.Recommanded Product: 4-Ethyl-piperazine-1-carbonyl chloride

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On January 25, 2000, Folkman, Moses J.; Ingber, Donald; Fujita, Takeshi published a patent.Application of 53788-12-8 The title of the patent was Preparation of O-substituted fumagillol derivatives with angiogenesis inhibitory activity. And the patent contained the following:

This invention relates to the preparation and use of O-substituted fumagillol derivatives of formula I [R1 = (substituted) 2-methyl-1-propenyl, (substituted) isobutyl; R2 = alkanoyl, aroyl, aromatic heterocycle-carbonyl, carbamoyl, alkyl, alkylsulfonyl, alkoxycarbonyl, etc.], or salts thereof preferably, O-(N-chloroacetylcarbamoyl)fumagillol, O-(N-chloroacetylcarbamoyl)dihydrofumagillol or O-(N-chloroacetylcarbamoyl)-6’b-hydroxyfumagillol, which have angiogenesis inhibitory activity, in the treatment and prevention of various diseases caused or advanced by abnormally hyperactive angiogenesis, especially various inflammatory diseases (rheumatism, psoriasis, etc.), diabetic retinopathy and cancer and other angiogenesis-dependent tumors, especially Kaposi’s sarcoma, breast cancer, colon cancer. Thus, II (AGM-1470) was prepared from fumagillol and chloroacetyl isocyanate in 71% yield. The T/C ratio of II in the B16 mouse melanoma model was 0.47 after 2 wk and 0.20 after 3 wk. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Application of 53788-12-8

The Article related to fumagillol derivative preparation angiogenesis inhibitor, kaposi sarcoma treatment fumagillol derivative preparation, breast cancer treatment fumagillol derivative preparation, antitumor fumagillol derivative preparation and other aspects.Application of 53788-12-8

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On August 18, 1975, there was a patent about cycloaddition reaction.Recommanded Product: 53788-12-8 The title of the patent was p-Dithiino[2,3-c]pyrroles. And the patent contained the following:

Dithiinopyrroles I (R = OH, OMe, R1 = H; R = Me, R1 = H, Me, Cl, OMe; R = H, R1 = Cl, Me, OMe) were prepared by treating the 2-aminonaphthyridines with 5,6-dihydro-1,4-dithiin-2,3-dicarboxylic anhydride, chlorinating when R1 = OH, reducing the dithiinopyrroledione to the monohydroxy derivative, and treating the latter with chlorocarbonylpiperazines. II (R2 = Et, CHMe2, allyl, CH2CH2OH) were similarly prepared The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Recommanded Product: 53788-12-8

The Article related to dithiinopyrrolol piperazinecarboxylate naphthyridinyl pyridinyl, piperazinecarboxylate naphthyridinyldithiinopyrrolyl, pyridinyldithiinopyrrolyl piperazinecarboxylate, aminonaphthyridine dithiindicarboxylate condensation and other aspects.Recommanded Product: 53788-12-8

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On September 16, 2021, Ewin, Richard Andrew; Cox, Mark R.; Hot, Imelda; Bedore, Matthew W.; Respondek, Tomasz; Sheehan, Susan M.K. published a patent.Recommanded Product: 53788-12-8 The title of the patent was Preparation of heteroaryl azalide glycosides as immunomodulators. And the patent contained the following:

Defined herein are immunomodulating heteroaryl azalide glycosides I, stereoisomers thereof, and pharmaceutically acceptable salts thereof; wherein W is H, sugar residue; RingC is Ph, naphthyl, 5-6 membered monocyclic heteroaryl ring or 9-11 membered fused heteroaryl ring; R1 is substituted benzyl, CH2-heteroaryl; R2 is H, alkyl, acyl, substituted amide, alkylaryl, alkyl-heterocycle; R3 is alkyl, alkoxy, haloalkyl, haloalkoxy, alkyl-cycloalkyl, halogen, substituted amine, substituted amide, substituted sulfoxide, nitro, oxo, cyano, -C(O)H, acyl, carboxylate, oxo-carboxylate, OH, heterocyclic, heteroaryl; n is an integer 0-3; and pharmaceutically acceptable salts thereof; and compositions comprising said compounds Thus, heteroaryl azalide glycoside II was prepared The invention also includes methods for treating an inflammatory and/or immunol. disease or disorder in an animal by administering a therapeutically effective amount of compound, stereoisomer thereof, and a pharmaceutically acceptable salt thereof; or use of said compounds to prepare a medicament for treating an inflammatory and/or immunol. disease or disorder in an animal. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Recommanded Product: 53788-12-8

The Article related to polonovski demethylation aminoglycoside preparation human antiinflammatory, il1 cd163 tnf nfkb azithromycin macrolide aminoglycoside preparation human, immunomodulating hetero aryl tlr4 toll like receptor antiinflammatory and other aspects.Recommanded Product: 53788-12-8

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On February 1, 2017, Xiao, Ganyuan; Li, Yan; Qiang, Xiaoming; Xu, Rui; Zheng, Yunxiaozhu; Cao, Zhongcheng; Luo, Li; Yang, Xia; Sang, Zhipei; Su, Fu; Deng, Yong published an article.Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride The title of the article was Design, synthesis and biological evaluation of 4′-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer’s disease. And the article contained the following:

A series of 4′-aminochalcone-revastigmine hybrids were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer’s disease. The results showed that most of these compounds exhibited good multifunctional activities. In particular, compound 6c displayed the best inhibitory potency on acetylcholinesterase (IC50 = 4.91 μM), and significant antioxidative activity with a value 2.83-fold of Trolox. The kinetic anal. of AChE inhibition revealed that 6c showed mixed-type inhibition, binding simultaneously to the catalytic active site and peripheral anionic site of AChE. In addition, 6c inhibited self-induced Aβ1-42 aggregation and Cu2+-induced Aβ1-42 aggregation by 89.5% and 79.7% at 25 μM resp., as well as acted as a selective monoamine oxidase B inhibitor (IC50 = 0.29 μM) and a selective biometal chelator. Furthermore, 6c could cross the blood-brain barrier in vitro. Based on these results, Compound 6c could be considered as a very promising lead compound for Alzheimer’s disease. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride

The Article related to aminochalcone revastigmine hybrid synthesis blood brain barrier alzheimer disease, acetylcholinesterase inhibitors, alzheimer’s disease, aβ aggregation inhibitors, chalcone carbamate derivatives, monoamine oxidase b inhibitors, multifunctional agents and other aspects.Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On February 1, 2017, Xiao, Ganyuan; Li, Yan; Qiang, Xiaoming; Xu, Rui; Zheng, Yunxiaozhu; Cao, Zhongcheng; Luo, Li; Yang, Xia; Sang, Zhipei; Su, Fu; Deng, Yong published an article.Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride The title of the article was Design, synthesis and biological evaluation of 4′-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer’s disease. And the article contained the following:

A series of 4′-aminochalcone-revastigmine hybrids were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer’s disease. The results showed that most of these compounds exhibited good multifunctional activities. In particular, compound 6c displayed the best inhibitory potency on acetylcholinesterase (IC50 = 4.91 μM), and significant antioxidative activity with a value 2.83-fold of Trolox. The kinetic anal. of AChE inhibition revealed that 6c showed mixed-type inhibition, binding simultaneously to the catalytic active site and peripheral anionic site of AChE. In addition, 6c inhibited self-induced Aβ1-42 aggregation and Cu2+-induced Aβ1-42 aggregation by 89.5% and 79.7% at 25 μM resp., as well as acted as a selective monoamine oxidase B inhibitor (IC50 = 0.29 μM) and a selective biometal chelator. Furthermore, 6c could cross the blood-brain barrier in vitro. Based on these results, Compound 6c could be considered as a very promising lead compound for Alzheimer’s disease. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride

The Article related to aminochalcone revastigmine hybrid synthesis blood brain barrier alzheimer disease, acetylcholinesterase inhibitors, alzheimer’s disease, aβ aggregation inhibitors, chalcone carbamate derivatives, monoamine oxidase b inhibitors, multifunctional agents and other aspects.Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics