A method is described of resolving a racemic bicycloheptenone of formula (1)
(in which X is a hydrogen, chlorine or bromine atom) which comprises forming an a-hydroxysulphonic acid - chiral amine salt thereof of formula (2)
(in which A is the chiral amine), separating the diastereomeric salts and regenerating the bicycloheptenone of formula (1) in optically active form from the separated salt.
The resolved bicycloheptenones are useful in the stereospecific synthesis of prostanoids and other substituted cyclopentanones.
描述了一种解析式(1)外消旋双环庚烯酮(其中 X 为氢、氯或溴原子)的方法,该方法包括形成式(2)a-羟基磺酸-手性胺盐(其中 A 为手性胺),分离非对映盐并从分离盐中再生出光学活性形式的式(1)双环庚烯酮。 解析出的双环庚烯酮可用于前列腺素和其他取代的环戊酮的立体特异性合成。
Preparation of aminocyclopentanealkenoic acids
申请人:GLAXO GROUP LIMITED
公开号:EP0078668A1
公开(公告)日:1983-05-11
A process is described for the preparation of compounds of the formula (1)
(and their salts and hydrates) in which:
W is alkylene
X is cis or trans-CH=CH-;
Y is a saturated heterocyclic amino group having 5-8 ring members; and
R2 is C3-6 alkenyl (optionally substituted), C1-12 alkyl, or substituted or unsubstituted phenylalkyl, thienylalkyl, furanylalkyl, biphenylalkyl or naphthylalkyl.
The process comprises hydrolysing an ester of the acid (1).
描述了一种制备式(1)化合物(及其盐和水合物)的工艺,其中
(及其盐类和水合物)的工艺,其中
W 是亚烷基
X 是顺式或反式-CH=CH-;
Y 是具有 5-8 个环成员的饱和杂环氨基;以及
R2 是 C3-6 烯基(任选取代)、C1-12 烷基或取代或未取代的苯基烷基、噻吩基烷基、呋喃基烷基、联苯基烷基或萘基烷基。
该工艺包括水解酸 (1) 的酯。
Aminocyclopentane esters and their preparation and pharmaceutical formulation
申请人:GLAXO GROUP LIMITED
公开号:EP0074861A1
公开(公告)日:1983-03-23
Compounds are described of the formulae
in which
-COR1 is a complex ester or thioester group,
W is alkylene,
X is cis or trans -CH=CH or -CH2CH2-,
n is 1 or 2,
Y is a saturated heterocyclic amino group having 5 - 8 ring
members, and
R2 is unsubstituted or substituted phenylalkyl, thienylalkyl,
naphthylalkyl or cinnamyl,
and their salts and solvates.
These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and antiasthmatic agents.
Method for the improvement of cyclosporine therapy
申请人:MERCK FROSST CANADA INC.
公开号:EP0300675A2
公开(公告)日:1989-01-25
The present invention relates to a method for improving cyclosporine therapy, in particular a method for limiting cyclosporine induced nephrotoxicity which comprises the adjunct administration in a mammal of an effective amount of cyclosporine and an effective amount of an antithromboxane A₂ agent.
Use of thromboxane A2 antagonists for the manufacture of a medicament for improving post-ischemic myocardial dysfunction
申请人:E.R. Squibb & Sons, Inc.
公开号:EP0309801A2
公开(公告)日:1989-04-05
A method is provided for improving post-ischemic myocardial dysfunction such as contractile dysfunction or reperfusion injury by administering a thromboxane A₂ antagonist before, during or immediately after an ischemic attack.