樟腦衍生化合物及其製造方法與應用Camphor-derived β-amino Alcohol Compounds, Method For Manufacturing The Same and Asymmetric Addition Of Organozinc To Aldehydes Using The Same

專利類型

發明

專利國別 (專利申請國家)

美國

專利申請案號

12/818,738

專利證號

US 8,309,715 B2

專利獲證名稱

樟腦衍生化合物及其製造方法與應用Camphor-derived β-amino Alcohol Compounds, Method For Manufacturing The Same and Asymmetric Addition Of Organozinc To Aldehydes Using The Same

專利所屬機關 (申請機關)

國立清華大學

獲證日期

2012/11/13

技術說明

本發明係關於一種對亞胺(imines)進行鏡像選擇性加成(enantioselective addition)之方法，尤指一種使用掌性β-胺基醇對亞胺進行有機鋅鏡像選擇性加成之方法。掌性胺類分子於合成生物活性物質及藥物扮演極為重要的角色，例如，甲氧那明(methoxyphenamine)為β2-腎上腺素的對抗藥，能治療氣喘;卡巴拉汀(rivastigmine)為假性不可逆之膽鹼酶抑制劑，能治療阿茲海默症;另外坦索洛新(tamsulosin)是一種選擇性的α1-腎上腺素的阻斷劑，能治療攝護腺腫大所造成的泌尿性問題;瑞格列奈(repaglinide)則是能刺激胰腺釋放胰島素，進而降低血糖濃度，為第二型糖尿病藥物。據此，發展一種可合成出具有高純度光學活性之胺類分子產物的方法係本發明之重要目標。 The present invention relates to a method of enantioselective addition to imines and, more particularly, to a method of enantioselective addition of organozinc to imines using a chiral β-amino alcohol. Chiral amines play important roles in synthesis of bioactive substances and drugs. For example, methoxyphenamine is a β-adrenergic receptor agonist and can be used to treat asthma; rivastigmine is a pseudo-irreversible inhibitor of cholinesterase and can be used to treat Alzheimer's disease; tamsulosin is a selective α1-adrenoceptor antagonist and can be used to decrease urinary symptoms caused by prostate hypertrophy; and repaglinide can stimulate the release of insulin from the pancreas to reduce blood glucose and thus can be used in treating treating type II diabetes. Accordingly, it is an important object of the present invention to develop a method for preparing amine products in high optical purity.

備註

本部(收文第1080013912號)108年03月04日清智財字第1089001408號所報專利終止維護案。

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