CAS: 142253-55-2; N-Boc-Azetidine-3-Carboxylic Acid

该化合物是一种保护性乙酰衍生物,它含有一种加强合成应用期间稳定性和处理的乙型丁氧碳酸(Boc)组,在合成过程中可加强稳定性和处理;该化合物是有机合成的多功能构件,特别是在Peptide和药用化学中,可以有选择地在温酸条件下将乙基类有选择地去除;其僵硬的醋酸环有助于目标分子的相容性限制,有可能改善绑定的亲和代谢稳定性;氨基酸功能允许通过恐吓或酯化进一步衍生;这种试剂因其纯度,一贯性,与广泛反应条件的兼容性而受到重视.

结构式图片

相似化合物

193693-64-0 36476-78-5 875629-26-8

欧盟法规

ECHA物质C&L通报

上下游产品

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合成工艺路线路线简述

  • 合成目标产物 1-N-Boc-3-Azetidinecarboxylic Acid 主要起始原料 Di-Tert-Butyl Dicarbonate And 3-Azetidinecarboxylic Acid
  • (文献来源)合成步骤主要原料 Di-Tert-Butyl Dicarbonate 和 3-Azetidinecarboxylic Acid
1-Boc-3-碘氮杂环丁烷置于sodium Hydroxide体系中,用 甲醇,水,二甲基亚砜 用作溶剂,化学反应 10.0H,反应生成1-N-Boc-3-吖丁啶羧酸
参考文献:受保护的 3-卤代氮杂环丁烷的改进的克级合成:氮杂环丁烷-3-羧酸的快速多样化合成
标题:受保护的 3-卤代氮杂环丁烷的改进的克级合成:氮杂环丁烷-3-羧酸的快速多样化合成
摘要:氮杂环丁烷是在各种天然产物和药物化合物中发现的越来越重要的杂环.受保护的 3-卤代氮杂环丁烷是药物化学中广泛使用的通用构件,已在 1-氮杂双环 [1.1.0] 丁烷的一锅,克级应变释放反应中从市售原料制备.这些中间体随后用于制备一系列高价值的氮杂环丁烷-3-羧酸衍生物,包括首次报道的 1-(叔丁氧基羰基)-3-((三氟甲基)硫代)氮杂环丁烷-3-羧酸的合成.
Doi:10.24820/ark.5550190.P010.549

海关参考信息

专利信息


专利号:US-2025091989-A1
优先权日:2023-09-19
标 题 :Small molecule protein synthesis modulators
发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE
权利人:INTERDICT BIO INC
摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.

专利号:US-7816375-B2
优先权日:2000-09-11
标 题 :Ligands for monoamine receptors and transporters, and methods of use thereof
发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HOLLAND JOANNE M; PERSONS PAUL E; RADEKE HEIKE; WANG FENGJIANG; SHAO LIMING
权利人:SEPRACOR INC
摘要:One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

专利号:US-9676783-B2
优先权日:2008-10-22
标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds
发明人:HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN
权利人:ARRAY BIOPHARMA INC
摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.

专利号:US-8697888-B2
优先权日:2012-01-06
标题 :Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors
发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; CHEUNG YIU-YIN
权利人:UNIV VANDERBILT
摘要:In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

专利号:US-8772301-B2
优先权日:2009-12-18
标题 :Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
发明人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D
权利人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D; SUNOVION PHARMACEUTICALS INC
摘要:Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

专利号:US-2009170828-A1
优先权日:2006-06-12
标题:Azetidine Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase
发明人:ISABEL ELISE; OBALLA RENATA; POWELL DAVID; ROBICHAUD JOEL
权利人:ISABEL ELISE; OBALLA RENATA; POWELL DAVID; ROBICHAUD JOEL
摘要:Azetidine derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis. (I)
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主要参考文献

[参考文献]: Beck A, Et Al. Strategies And Challenges For The Next Generation Of Antibody-Drug Conjugates. Nat Rev Drug Discov. 2017;16(5):315-337.
[参考文献]: Nalawansha Da, Et Al. Protacs: An Emerging Therapeutic Modality In Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.

合成参考文献


摘要:Li, Y.; Fang, X.; Wang, Y., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 24.
摘要:Dong, X.; Qin, H.; Chen, Y., Science of Synthesis: Hypervalent Halogens in Organic Synthesis, (2025) .
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