公开(公告)号：US6143900A

公开(公告)日：2000-11-07

申请号：US426778

申请日：1999-10-26

申请人： Won Hun Ham ,  Kyung Seok Choi ,  Han Won Lee ,  Sung Ki Seo ,  Jin Kyu Park ,  Ki Young Lee ,  Yong Hyun Kim

发明人： Won Hun Ham ,  Kyung Seok Choi ,  Han Won Lee ,  Sung Ki Seo ,  Jin Kyu Park ,  Ki Young Lee ,  Yong Hyun Kim

IPC分类号： C07C231/12 ,  C07C233/71 ,  C07D263/10 ,  C07D263/12 ,  C07D305/14 ,  C07D263/34

CPC分类号： C07D263/10 ,  C07C231/12 ,  C07C233/71 ,  C07D263/12 ,  C07D305/14 ,  C07B2200/07

摘要： The present invention relates to stereoselective synthetic method of oxazoline derivative. More particularly, it relates to a synthetic method of oxazoline derivative having the structure of formula I. ##STR1## wherein R represents phenyl, benzyl, methyl, ethyl, isopropyl, isobutyl, cyclohexyl or cyclohexylmethyl.

摘要翻译： 本发明涉及恶唑啉衍生物的立体选择性合成方法。 更具体地说，本发明涉及具有式I结构的恶唑啉衍生物的合成方法，其中R表示苯基，苄基，甲基，乙基，异丙基，异丁基，环己基或环己基甲基。

公开(公告)号：US6127546A

公开(公告)日：2000-10-03

申请号：US515591

申请日：2000-02-29

申请人： Jin Kyu Park ,  Kyung Seok Choi ,  Han Won Lee ,  Sung Ki Seo ,  Won Hun Ham ,  Chang Young Oh ,  Kee Young Lee ,  Yong Hyun Kim ,  Min Sung Park

发明人： Jin Kyu Park ,  Kyung Seok Choi ,  Han Won Lee ,  Sung Ki Seo ,  Won Hun Ham ,  Chang Young Oh ,  Kee Young Lee ,  Yong Hyun Kim ,  Min Sung Park

IPC分类号： C07D263/14 ,  B01J31/24 ,  C07B61/00 ,  C07D233/54 ,  C07D263/12 ,  C07D263/16

CPC分类号： C07D233/64

摘要： The present invention relates to a process for the preparation of an oxazoline compound which is easily chemically converted to a beta-amino-alpha-hydroxy acid or a gamma-amino-beta-hydroxy acid. The method comprises producing a compound of the following formula (4) using .alpha.-amino acid. The produced compound (4) is subjected to an intramolecular cyclization to produce an oxazoline compound of the following formula (3). The oxazoline compound (3) is oxidized at a vinyl group with RuCl.sub.3 or NaIO.sub.4 to produce an oxazoline compound of the following formula (1) which is easily chemically converted to a beta-amino-alpha-hydroxy acid. Alternatively, the oxazoline compound (3) may also be treated with 9-borabiclo[3.3.1]nonane such that a hydroxy group is introduced into the end of the vinyl group of the oxazoline compound(3). The introduced end hydroxy group is oxidized with RuCl.sub.3 or NaIO.sub.4 to produce an oxazoline compound of the following formula (2) which is easily chemically converted to a gamma-amino-hydroxy acid.

摘要翻译： 本发明涉及一种易于化学转化为β-氨基-α-羟基酸或γ-氨基-β-羟基酸的恶唑啉化合物的制备方法。 该方法包括使用α-氨基酸制备下式（4）的化合物。 将所制备的化合物（4）进行分子内环化，得到下式（3）的恶唑啉化合物。 恶唑啉化合物（3）用乙烯基用RuCl 3或NaIO 4氧化，得到容易化学转化为β-氨基-α-羟基酸的下式（1）的恶唑啉化合物。 或者，恶唑啉化合物（3）也可以用9-硼烷[3.3.1]壬烷处理，使得羟基被引入到恶唑啉化合物（3）的乙烯基的末端。 引入的末端羟基用RuCl 3或NaIO 4氧化以产生下式（2）的恶唑啉化合物，其易于化学转化为γ-氨基 - 羟基酸。