专利号:US-8865935-B2 优先权日:2011-06-30 标题:Purification methods for betulonic acid and Boc-lysinated betulonic acid, and organic synthesis of betulonic acid amides with piperazine derivatives 发明人:CHUE KUCK-TACK; KIM TAE-HWAN; TEN LEONID 权利人:CHUE KUCK-TACK; KIM TAE-HWAN; TEN LEONID; KOREA ENERGY RESEARCH INST 摘要:The present invention provides a method of purifying betulonic acid contained the reaction product of organic synthesis of a Jones oxidation reagent and betulin extracted from the bark of a birch, a method of preparing a piperazine betulonic acid amide derivative, which is used as a chemical having an antibacterial function, using the high-purity betulonic acid obtained by the purification method and a derivative prepared by this method, a method of purifying a Boc-lysinated betulonic acid monomer ester contained in the reaction product of organic synthesis of lysine and the high-purity betulonic acid (starting material) obtained by the purification method, and a method of purifying Boc-lysinated betulonic acid contained in the reaction product of hydrolysis of the high-purity Boc-lysinated betulonic acid monomer ester.
专利号:US-2009131714-A1 优先权日:2005-06-08 标题:Synthesis of betulonic and betulinic aldehydes 发明人:KRASUTSKY PAVEL A; MUNSHI KALYAN 权利人:KRASUTSKY PAVEL A; MUNSHI KALYAN 摘要:The present invention provides for methods of selectively converting betulin to betulonic aldehyde. The present invention also provides for methods of selectively converting 3-substituted triterpen-28-ols to the corresponding 3-substituted triterpen-28-carboxaldehydes. Additionally, the present invention provides for methods of preparing betulonic aldehyde, betulonic acid, betulinic acid, and corresponding 3-substituted triterpenes.
专利号:US-8969395-B2 优先权日:2009-05-20 标题 :Triterpenoid derivatives useful as antiproliferative agents 发明人:RIBEIRO SALVADOR JORGE ANTONIO; MENDES DOS SANTOS RITA CATARINA; CASCANTE SERRATOSA MARTA 权利人:RIBEIRO SALVADOR JORGE ANTONIO; MENDES DOS SANTOS RITA CATARINA; CASCANTE SERRATOSA MARTA; UNIV DE COIMBRA 摘要:Formula (I) and (II). The present invention relates to the use of a new lupane derivative of general formula (I) or (II), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, for preventing and/or inhibiting tumor growth and for treating cancer and other proliferative diseases, more particularly for treating leukemia, liver, cervical, colon and prostate cancer. The present invention also relates to the synthesis of these compounds and to pharmaceutical compositions which contain them.
专利号:RU-2190622-C1 优先权日:2001-12-26 标 题 :Method of synthesis of betulinic acid
专利号:US-2014243527-A1 优先权日:2011-06-30 标题:Purification methods for betulonic acid and boc-lysinated betulonic acid, and organic synthesis of betulonic acid amides with piperazine derivatives
专利号:WO-2006133314-A2 优先权日:2005-06-08 标 题:Synthesis of betulonic and betulinic aldehydes
参考标题:Expedient Synthesis Of Alphitolic Acid And Its Naturally Occurring 2-O-Ester Derivatives 作者:Somin Park,Jihee Cho,Hongjun Jeon,Sang Hyun Sung,Seunghee Lee,Sanghee Kim |发布日期:2019.4.26 摘要:Expedient Synthesis Of Alphitolic Acid (1) As Well As Its Natural C-3-Epimer And 2- O-Ester Derivatives Was Accomplished In A Few Steps From The Readily Commercially Available Betulin (9). A Rubottom Oxidation Delivered An α-Hydroxy Group In A Stereo- And Chemoselective Manner. The Diastereoselective Reduction Of The α-Hydroxy Ketone Was Key To Accessing The 1,2-Diol Moiety Of This Class Of Natural Products
合成参考文献
参考文献:10.1016/s0960-894x(01)00460-7 摘要:Kim JY, Koo H, Kim DSHL. Development of C-20 modified betulinic acid derivatives as antitumor agents. Bioorganic & Medicinal Chemistry Letters. 2001 Sep;11(17):2405–8. doi: 10.1016/s0960-894x(01)00460-7. 参考文献:10.1016/j.bmcl.2004.04.010|10.1016/s0960-894x(04)00491-3 摘要:Mukherjee R, Jaggi M, Rajendran P, Srivastava SK, Siddiqui MJA, Vardhan A, Burman AC. Synthesis of 3-O-acyl/3-benzylidene/3-hydrazone/3-hydrazine/17-carboxyacryloyl ester derivatives of betulinic acid as anti-angiogenic agents. Bioorganic & Medicinal Chemistry Letters. 2004 Jun;14(12):3169–72. doi: 10.1016/j.bmcl.2004.04.010. 参考文献:10.1016/j.bmc.2006.05.048 摘要:Saxena BB, Zhu L, Hao M, Kisilis E, Katdare M, Oktem O, Bomshteyn A, Rathnam P. Boc-lysinated-betulonic acid: a potent, anti-prostate cancer agent. Bioorg Med Chem. 2006 Sep 15;14(18):6349–58. doi: 10.1016/j.bmc.2006.05.048. 参考文献:10.1007/s10517-005-0490-0 摘要:Zhukova NA, Semenov DE, Sorokina IV, Tolstikova TG, Pozdnyakova SV, Grek OR. Effect of Betulonic Acid and Its Derivative [3-Oxo-20(29)-Lupene-28-Oyl]-3-Aminopropionic Acid on Liver Structure in Mice with RLS Lymphoma. Bulletin of Experimental Biology and Medicine. 2005 Sep;140(3):361–4. doi: 10.1007/s10517-005-0490-0. 参考文献:10.1038/ja.2010.2 摘要:Alakurtti S, Bergström P, Sacerdoti-Sierra N, Jaffe CL, Yli-Kauhaluoma J. Anti-leishmanial activity of betulin derivatives. J Antibiot (Tokyo). 2010 Mar;63(3):123–6. doi: 10.1038/ja.2010.2.