合成目标产物 Tadalafil 主要起始原料 Methylamine And Chloropretadalafil
(文献来源)合成步骤主要原料 Methylamine 和 Chloropretadalafil
胡椒醛置于三乙胺体系中,用 四氢呋喃,水 用作溶剂,化学反应 3.25H,反应生成他达那非 参考文献:Process For Obtaining Compounds Derived From Tetrahydro-Beta-Carboline 标题:Process For Obtaining Compounds Derived From Tetrahydro-Beta-Carboline 摘要:该发明涉及一种从四氢-β-咔啉衍生的化合物获得过程,具体包括从合成中得到的他达拉非和中间产物,其中包括对间茴香醛和d-色氨酸烷基酯作为盐之间的反应,无其他成分参与,然后进行卤乙酰化和最终与甲胺进行环化反应.
专利号:US-10633360-B2 优先权日:2014-12-23 标题 :Efficient process for the synthesis of alkoxy substituted benzaldehydes 发明人:MOHAPATRA Manoj Kumar; BENDAPUDI Ramamohanrao; MENACHERRY Paul Vincent; PAUL VINCENT 权利人:ANTHEA AROMATICS PRIVATE LTD 摘要:The present invention relates to the synthesis of alkoxy substituted benzaldehydes obtained from the corresponding alkoxy substituted benzenes. Alkoxy substituted benzaldehydes are products of broad commercial interest and are used as end products and intermediates in flavor and fragrance applications and pharmaceutical ingredients. For example, 3,4-methylendioxy-benzaldehyde (also known as heliotropin or piperonal) is used widely both as a end product and intermediate for the above mentioned applications. Other examples include 3,4-dimethoxybenzaldehyde, 3,4,5-trimethoxybenzaldehyde and 3,4-ethylenedioxybenzene which are intermediates in the synthesis of active pharmaceutical intermediates.
专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-2022356139-A1 优先权日:2019-09-03 标 题:Synthesis of deuterated aldehydes 发明人:WANG WEI 权利人:ARIZONA BOARD OF REGENTS ON BEHALF OF ATHE UNIV OF ARIZONA 摘要:Described are methods for preparing a deuterated aldehyde using N-heterocyclic carbene catalysts in a solvent comprising D 2 O. The methods may be used to convert a wide variety of aldehydes (e.g., aryl, alkyl, or alkenyl aldehydes) to C-1 deuterated aldehydes under mild reaction conditions without functionality manipulation.
专利号:US-2024082118-A1 优先权日:2021-05-19 标 题:Topical compositions and methods of preparing the same 发明人:ABRAMOVICH SAGI; AVIDOR GAL; LANDA BENZION 权利人:LANDA LABS 2012 LTD 摘要:There is disclosed a composition comprising a water-insoluble thermoplastic compound capable of stimulating collagen synthesis (CSSC), the CSSC having a molecular weight of more than 0.6 kDa and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less and a viscosity of 107 mPa·s or less. The nano-elements of CSSC can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon their application to a surface to be treated therewith. Methods for preparing the compositions and uses thereof are also provided.
专利号:US-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
专利号:US-12295961-B2 优先权日:2009-12-31 标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols 发明人:DHINGRA OM 权利人:MARIUS PHARMACEUTICALS INC 摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
1: Henrie AM, Nawarskas JJ, Anderson JR. Clinical utility of tadalafil in the treatment of pulmonary arterial hypertension: an evidence-based review. Core Evid. 2015 Nov 2;10:99-109. doi: 10.2147/CE.S58457. eCollection 2015. Review. 2: Yokoyama O, Igawa Y, Takeda M, Yamaguchi T, Murakami M, Viktrup L. Tadalafil for lower urinary tract symptoms secondary to benign prostatic hyperplasia: a review of clinical data in Asian men and an update on the mechanism of action. Ther Adv Urol. 2015 Oct;7(5):249-64. doi: 10.1177/1756287215589238. Review. 3: Kadıoğlu A, Ortaç M, Dinçer M, Brock G. Tadalafil therapy for erectile dysfunction following prostatectomy. Ther Adv Urol. 2015 Jun;7(3):146-51. doi: 10.1177/1756287215576626. Review.
合成参考文献
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