专利号:WO-2021014395-A1 优先权日:2019-07-24 标题:Process for the synthesis of deuterated capsaicin, capsaicinoids and synthetic capsaicin analogs 发明人:ORUGANTI SRINIVAS; AMRUTAPU SRAVANTH KUMAR; SAMPATH MAGESH; SEN SAIKAT 权利人:DR REDDY’S INST OF LIFE SCIENCES 摘要:The present application provides novel processes for the synthesis of deuterated intermediates of capsaicinoids, particularly II, III, IV and V of capsaicinoids, relating to pharmaceutical applications. The invention also provides novel intermediates of compounds of formula IX, XIV, XV, XVI, XVII, XVIII, XX and XXI utilized in the process of making deuterated capsaicin II, III, IV and V.
专利号:US-2025051339-A1 优先权日:2021-12-15 标题:Methods for the synthesis of complement factor d inhibitors 发明人:HASHIMOTO AKIHIRO 权利人:ALEXION PHARMA INC 摘要:The present disclosure provides methods for the synthesis of complement factor D inhibitors and intermediates thereof. The methods involve subjecting an intermediate in the synthesis of a complement factor D inhibitor to a t-butyl ester deprotection reaction using a weak base.
专利号:US-2007259917-A1 优先权日:2006-04-24 标题 :Processes for the synthesis of 3-isobutylglutaric acid 发明人:KANSAL VINOD K; CHAURASIA BRIJNATH P; PATEL HITESH K; SHELKE SHIVAJI H; MORE YOGESH P 权利人:KANSAL VINOD K; CHAURASIA BRIJNATH P; PATEL HITESH K; SHELKE SHIVAJI H; MORE YOGESH P 摘要:Provided are processes for the synthesis of 3-isobutylglutaric acid, an intermediate in the synthesis of (S)-Pregabalin.
专利号:WO-2024055132-A1 优先权日:2022-09-12 标 题 :Method for the synthesis of a branched copolymer of hyaluronic acid and poly(lactic-co-glycolic) acid 发明人:VILOS ORTIZ CRISTIAN ANDRÉS; ZACCONI FLAVIA CRISTINA MILAGRO; SALAZAR MUÑOZ JAVIER ALONSO 权利人:UNIV TALCA; UNIV PONTIFICIA CATOLICA CHILE; FUND CENTRO DE NANOCIENCIA Y NANOTECNOLOGIA 摘要:The present invention provides a method for the synthesis of a branched copolymer of hyaluronic acid (HA) and poly(lactic-co-glycolic acid) (PLGA), and the branched copolymer thus obtained (HA-g-PLGA). Said method comprises activating the PLGA with coupling reagents in a water miscible solvent; solubilizing the HA in a phosphate buffered saline solution; and adding the activated PLGA solution dropwise to the solution with HA to obtain the branched copolymer. The advantages of the present method are that it uses environmentally friendly conditions and allows the copolymer to be synthesized and purified in less than a week under laboratory conditions. In addition, the branched copolymer obtained does not present traces of any of the reagents used for its synthesis, so it can be used directly in the development of applications for human use.
专利号:US-8901352-B2 优先权日:2011-01-13 标题 :Method for the synthesis of rasagiline 发明人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN 权利人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN; NOBEL ILAÇ SANAYII VE TICARET A S 摘要:We have developed a new method for the synthesis of Rasagiline (Formula 1) based on the alkylation of trifluoroacetyl protected aminoindan. This protection enabled us to carry out an alkylation of aminoindan with a high yield and purity under very mild conditions with a wide range of reaction conditions and reagent selection. Considering the ease, purity and high yields of introducing and removal of the trifluoroacetyl group, this approach is a highly practical and economical way for the synthesis of rasagiline or its pharmaceutically acceptable salts.
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.