CAS: 106089-24-1; Methacryloyl-D-Proline

该化合物是氮位置上2-甲基-1-oxo-2-propenyl组的活性派生衍生物,这种改变增强了其在不对称合成和peptide化学中的效用,在这种化学中,僵硬的阳利丁环和立体化学纯度是有利的.该化合物的结构特征使得它对于设计酶抑制剂,催化剂和生物活性peptime很有价值.它的高度对应性纯度保证了合成应用中精确的立体控制,而类似丙烯基质的子成份则为进一步的功能化提供了再活动性. 这种衍生物在医药化学和材料科学中特别有用,因为先进的研究和开发需要量制成的准仿真物.

结构式图片

相似化合物

1074-79-9 68-95-1 59785-68-1

上下游产品

D-Prolin Methacryloyl chloride tert-butyl methyl ether 1-(2-methyl-1-oxo-2-propenyl)pyrrolidine c][1,4]oxazine-1,4-dione3-bromomethyl-3-methyl-tetrahydro-pyrrolo[2,1-c][1,4]oxazine-1,4-dione (3R,8AR)-3-Bromomethyl-3-methyl-tetrahydro-pyrrolo[2,1-c][1,4]oxazine-1,4-dione (3R,8R)-3-Bromomethyl-3-methyl-tetrahydropyrolo[2,1-c][1,4]oxazine-1,4-dione (2R)-3-bromo-2-hydroxy-2-methylpropanoic acid

合成工艺路线路线简述

  • 合成目标产物 (R)-1-Methacryloylpyrrolidine-2-Carboxylic Acid 主要起始原料 D-Proline And Methacryloyl Chloride
  • (文献来源)合成步骤主要原料 D-Proline 和 Methacryloyl Chloride

海关参考信息

专利信息


专利号:US-7759520-B2
优先权日:1996-11-27
标 题 :Synthesis of selective androgen receptor modulators
发明人:DALTON JAMES T; MILLER DUANE D; YIN DONGHUA; HE YALI
权利人:UNIV TENNESSEE RES FOUNDATION
摘要:The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.

专利号:US-6995284-B2
优先权日:2000-08-24
标题 :Synthesis of selective androgen receptor modulators
发明人:DALTON JAMES T; MILLER DUANE D; HE YALI; YIN DONGHUA
权利人:UNIV TENNESSEE RES FOUNDATION
摘要:The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.

专利号:US-7968721-B2
优先权日:2003-01-13
标 题:Large-scale synthesis of selective androgen receptor modulators
发明人:MILLER DUANE D; VEVERKA KAREN A; CHUNG KIWON
权利人:UNIV TENNESSEE RES FOUNDATION
摘要:This invention relates to a process for preparing a selective androgen receptor modulator (SARM) compound represented by the structure of formula I: n nwherein X is O; and T, Z, Y, Q, R and R 1 are defined herein. The process includes coupling between an amide of formula II and a phenol of formula IIIn n n n n n n n n n n nfollowed by a purification step consisting of precipitating the compound of formula (I) in a mixture of alcohol and water alone.

专利号:US-2004014975-A1
优先权日:2000-08-24
标 题:Synthesis of selective androgen receptor modulators

专利号:US-2006009529-A1
优先权日:1996-11-27
标 题:Synthesis of selective androgen receptor modulators

专利号:ES-2420129-T3
优先权日:2003-01-13
标题 :Large-scale synthesis of selective androgen receptor modulators

供应商参考报价(招募中)

品牌试剂参考报价(招募中)

📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

合成参考文献


参考文献:10.1055/a-1845-9291
摘要:Sani M, Zanda M. Recent Advances in the Synthesis and Medicinal Chemistry of SF5 and SF4Cl Compounds. Synthesis. 2022 Jun 21;54(19):4184–209. doi: 10.1055/a-1845-9291.
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