7-羧基吲哚啉置于palladium On Activated Charcoal体系中,用 Xylene 用作溶剂,化学反应 4.0H,以52%的收率获得7-吲哚甲酸 参考文献:Synthesis And Evaluation Of Heterocyclic Carboxamides As Potential Antipsychotic Agents 标题:Synthesis And Evaluation Of Heterocyclic Carboxamides As Potential Antipsychotic Agents 摘要:Heterocyclic Analogues Of 1192U90,2-Amino-N-(4-(4-(1,2-Benzisothiazol-3-yl)-1-Piperazinyl)-Butyl)Benzamide Hydrochloride (1),Were Prepared And Evaluated As Potential Antipsychotic Agents. These Analogues Were Evaluated In Vitro For Their Binding To The Dopamine D-2,Serotonin 5-Ht2,And Serotonin 5-Htl(1A) Receptors And In Vivo For Their Ability To Antagonize The Apomorphine-Induced Climbing Response In Mice. Nine Different Types Of Heterocyclic Carboxamides Were Studied In This Investigation (I.E.,Pyridine-,Thiophene-,Benzothiophene-,Quinoline-,1,2,3,4-Tetrahydroquinoline-,2,3-Dihydroindole-,Indole-,Benzimidazole-,And Indazolecarbox-Amides),Two Derivatives Exhibited Potent In Vivo Activities Comparable To 1: 3-Amino-N-(4-(4-(1,2-Benzisothiazol-3-yl)-1-Piperazinyl)Butyl)-2-Pyridinecarboxamide (16) And 3-Amino-N-(4-(4-(1,2-Benzisothiazol-3-yl)-1-Piperazinyl)Butyl)-2-Thiophenecarboxamide (29). Furthermore,These Derivatives Were Found To Be Much Less Active In Behavioral Models Predictive Of Extrapyramidal Side Effects Than In The Mouse Climbing Assay,Which Predicts Antipsychotic Activity. Carboxamides 16 And 29 Were Selected For Further Evaluation As Potential Backup Compounds To 1. Doi:10.1021/jm9603375
专利号:US-4841045-A 优先权日:1985-03-12 标 题 :Synthesis of vinblastine and vincristine type compounds 发明人:KUEHNE MARTIN 权利人:UNIV VERMONT 摘要:A new process for the stereospecific synthesis of alkaloids of the vinblastine and vincristine type including the synthesis of vinblastine and vincristine as well novel alkaloids which are active as anti-tumor agents.
专利号:US-4897477-A 优先权日:1985-03-12 标题:Synthesis of vinblastine and vincristine type compounds 发明人:KUEHNE MARTIN 权利人:UNIV VERMONT 摘要:A new process for the stereospecific synthesis of alkaloids of the vinblastine and vincristine type including the synthesis of vinblastine and vincristine as well novel alkaloids which are active as anti-tumor agents.
专利号:US-3983137-A 优先权日:1973-12-03 标题:Process for preparing 3-(indol-3-yl)-dehydronaphthalide hydrochlorides 发明人:CHIANG YUNN H 权利人:POLAROID CORP 摘要:This invention is concerned with a novel class of protonated compounds, namely, 3-(indol-3-yl)dehydronaphthalide hydrochlorides, with their synthesis by the reaction of a 3-(indol-3-yl)naphthalide and a high-potential quinone in an inert anhydrous aprotic solvent in the presence of a carboxylic acid catalyst, and with the synthesis of indole naphthalide indicator dyes by reacting the said dehydronaphthalide hydrochlorides and an indole in an aromatic hydrocarbon solvent in the presence of a carboxylic acid catalyst.
专利号:US-3933854-A 优先权日:1973-12-03 标题 :3-(Indol-3-yl)dehydronaphthalide hydrochlorides 发明人:CHIANG YUNN H 权利人:POLAROID CORP 摘要:This invention is concerned with a novel class of protonated compounds, namely, 3-(indol-3-yl)dehydronaphthalide hydrochlorides, with their synthesis by the reaction of a 3-(indol-3-yl)naphthalide and a high-potential quinone in an inert anhydrous aprotic solvent in the presence of a carboxylic acid catalyst, and with the synthesis of indole naphthalide indicator dyes by reacting the said dehydronaphthalide hydrochlorides and an indole in an aromatic hydrocarbon solvent in the presence of a carboxylic acid catalyst.
专利号:US-9056887-B2 优先权日:2011-07-26 标 题 :Minor groove binder phosphoramidites and methods of use 发明人:VOROBIEV ALEXEI; LUKHTANOV EUGENY A 权利人:VOROBIEV ALEXEI; LUKHTANOV EUGENY A; ELITECH HOLDING BV 摘要:Minor groove binder phosphoramidites having the formula M-L-PA, wherein M is a minor groove binder comprising a protected heteroaromatic amine, L is a linker, and PA is a phosphoramidite group, have been synthesized. Preferred methods of synthesis include synthesizing a minor groove binder intermediate containing a transiently protected hydroxyl group, protecting heteroaromatic amines of the corresponding minor groove binder intermediate as carbamate intermediates, reacting the carbamate intermediate to remove the transient protecting group to yield carbamate-protected minor groove binder agent as an intermediate with a free hydroxyl group, and converting the intermediate with a free hydroxyl group to the desired minor groove binder phosphoramidite. These minor groove binder phosphoramidites are useful in the preparation of oligonucleotide conjugates, particularly those for use as probes and primers. In preferred methods, an oligonucleotide sequence is synthesized using nucleoside phosphoramidites and the minor groove binder phosphoramidite is incorporated into the oligonucleotide sequence to form a protected oligonucleotide-minor groove binder conjugate. Then, deprotection produces the oligonucleotide-minor groove binder.
专利号:WO-8605491-A1 优先权日:1985-03-12 标 题 :Synthesis of vinblastine and vincristine type compounds