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1.发明授权Process for preparing intermediates for vitamin D derivatives and compounds obtained thereby 失效一种用于制备的中间体，用于维生素D衍生物和化合物的方法
公开(公告)号：EP0528209B1
公开(公告)日：1999-11-10
申请号：EP92112775.9
申请日：1992-07-27
IPC分类号： C07F7/18 , C07C401/00
CPC分类号： C07J9/00 , C07C401/00 , C07D333/72 , C07F7/1856 , C07F7/1892 , C07J51/00
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2.发明公开Intermediates for the synthesis of 3-epi vitamin D3 metabolites and analogs 审中-公开Zwischenprodukte zur Synthese von 3-epi Vitamin D3 Metaboliten und Analogen
公开(公告)号：EP0957098A1
公开(公告)日：1999-11-17
申请号：EP99108586.1
申请日：1999-05-06
IPC分类号： C07D303/16 , C07F9/53
CPC分类号： C07F9/532 , C07C401/00 , C07D303/16
摘要： Compounds of formulae
are usefull as intermediates in a process for the preparation of vitamin D 3 compounds of formula
wherein
A is a single or a double bond;
B is a single, cis-double, trans double or a triple bond;
R 1 and R 2 are independently hydrogen, a C 1 -C 4 alkyl;
R 3 and R 4 are independently a C 1 -C 4 alkyl, a hydroxyalkyl, and a haloalkyl.摘要翻译： 式
的化合物在制备式 的维生素D3化合物的方法中可用作中间体，其中A是单键或双键; B是单，顺 - 双，反式双键或三键; R1和R2独立地是氢，C1-C4烷基; R3和R4独立地是C1-C4烷基，羟基烷基和卤代烷基。 -
公开(公告)号：EP0808832A3
公开(公告)日：1999-02-03
申请号：EP97107868.8
申请日：1997-05-14
发明人： Manchand, Percy Sarwood , Nestor Jr., John Joseph , Uskokovic, Milan Radoje , Vickery, Brian Henry
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00 , C07F7/1856 , Y02P20/55
摘要： The novel fluorinated Vitamin D 3 analogs of formula
wherein:
X is (H,H) or =CH 2 ; R 1 and R2 are, independently of each other, hydrogen, (C 1 -C 4 ) alkyl or fluoroalkyl, or R 1 and R 2 together with C-20 form a (C 3 -C 6 ) cycloalkyl or cyclofluoroalkyl, or R 1 and R 2 together form =CH 2 ; R 3 and R 4 are, independently of each other, a (C 1 -C 4 ) alkyl or fluoroalkyl, or R 3 and R 4 together with C-25 form a (C 3 -C 9 ) cycloalkyl or cyclofluoroalkyl; A is a single bond or a double bond; and B is a double bond or a triple bond;
except that:
(i) when X is =CH 2 , R 3 and R 4 are each CF 3 , A is a double bond and one of R 1 or R 2 is hydrogen, then the other of R 1 or R 2 cannot be CH 3 ; (ii) when X is =CH 2 , R 3 and R 4 are each a (C 1 -C 2 ) alkyl, A is a double bond and R 2 is hydrogen, then R 1 cannot be CH 3 ; (iii) when X is =CH 2 , R 3 and R 4 are each a (C 1 -C 4 ) alkyl, A is a double bond and R 1 is hydrogen, then R 2 cannot be CH 3 ; (iv) when X is =CH 2 , one of R 3 or R 4 is a CF 3 , A is a double bond, R 1 is CH 3 and R 2 is hydrogen, then the other of R 3 or R 4 cannot be CH 3 ; and (v) when X is (H,H), R 3 and R 4 are each CF 3 , A is a double bond, B is a triple bond and R 2 is hydrogen, then R 1 cannot be CH 3 , and the compounds of the above formula I wherein: X is (H,H) or =CH 2 ; R 1 and R2 are, independently of each other, hydrogen, (C 1 -C 4 ) alkyl or fluoroalkyl, or R 1 and R 2 together with C-20 form a (C 3 -C 6 ) cycloalkyl or cyclofluoroalkyl, or R 1 and R 2 together form =CH 2 ; R 3 and R 4 are, independently of each other, a (C 1 -C 4 ) alkyl or fluoroalkyl, or R 3 and R 4 together with C-25 form a (C 3 -C 9 ) cycloalkyl or cyclofluoroalkyl; A is a single bond or a double bond; and B is a double bond or a triple bond; except that where R 3 and R 4 are each CF 3 and A is a double bond and B is a triple bond and R 2 is hydrogen, then R 1 cannot be CH 3 ,
are useful in the treatment of osteoporosis.-
公开(公告)号：EP0808832A2
公开(公告)日：1997-11-26
申请号：EP97107868.8
申请日：1997-05-14
发明人： Manchand, Percy Sarwood , Nestor Jr., John Joseph , Uskokovic, Milan Radoje , Vickery, Brian Henry
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00 , C07F7/1856 , Y02P20/55
摘要： The novel fluorinated Vitamin D 3 analogs of formula
wherein:
X is (H,H) or =CH 2 ;
R 1 and R2 are, independently of each other, hydrogen, (C 1 -C 4 ) alkyl or fluoroalkyl, or R 1 and R 2 together with C-20 form a (C 3 -C 6 ) cycloalkyl or cyclofluoroalkyl, or R 1 and R 2 together form =CH 2 ;
R 3 and R 4 are, independently of each other, a (C 1 -C 4 ) alkyl or fluoroalkyl, or R 3 and R 4 together with C-25 form a (C 3 -C 9 ) cycloalkyl or cyclofluoroalkyl;
A is a single bond or a double bond; and
B is a double bond or a triple bond;
except that:
(i) when X is =CH 2 , R 3 and R 4 are each CF 3 , A is a double bond and one of R 1 or R 2 is hydrogen, then the other of R 1 or R 2 cannot be CH 3 ;
(ii) when X is =CH 2 , R 3 and R 4 are each a (C 1 -C 2 ) alkyl, A is a double bond and R 2 is hydrogen, then R 1 cannot be CH 3 ;
(iii) when X is =CH 2 , R 3 and R 4 are each a (C 1 -C 4 ) alkyl, A is a double bond and R 1 is hydrogen, then R 2 cannot be CH 3 ;
(iv) when X is =CH 2 , one of R 3 or R 4 is a CF 3 , A is a double bond, R 1 is CH 3 and R 2 is hydrogen, then the other of R 3 or R 4 cannot be CH 3 ; and
(v) when X is (H,H), R 3 and R 4 are each CF 3 , A is a double bond, B is a triple bond and R 2 is hydrogen, then R 1 cannot be CH 3 ,
and the compounds of the above formula I wherein:
X is (H,H) or =CH 2 ;
R 1 and R2 are, independently of each other, hydrogen, (C 1 -C 4 ) alkyl or fluoroalkyl, or R 1 and R 2 together with C-20 form a (C 3 -C 6 ) cycloalkyl or cyclofluoroalkyl, or R 1 and R 2 together form =CH 2 ;
R 3 and R 4 are, independently of each other, a (C 1 -C 4 ) alkyl or fluoroalkyl, or R 3 and R 4 together with C-25 form a (C 3 -C 9 ) cycloalkyl or cyclofluoroalkyl;
A is a single bond or a double bond; and
B is a double bond or a triple bond;
except that where R 3 and R 4 are each CF 3 and A is a double bond and B is a triple bond and R 2 is hydrogen, then R 1 cannot be CH 3 ,
are useful in the treatment of osteoporosis.摘要翻译： 式
的新型氟化维生素D3类似物，其中：X为（H，H）或= CH 2; R 1和R 2彼此独立地为氢，（C 1 -C 4）烷基或氟代烷基，或者R 1和R 2与C 20一起形成（C 3 -C 6）环烷基或环氟烷基，或者R 1和R 2一起形成= CH 2; R 3和R 4彼此独立地为（C 1 -C 4）烷基或氟烷基，或者R 3和R 4与C-25一起形成（C 3 -C 9）环烷基或环氟烷基; A是单键或双键; B是双键或三键; 除了：（i）当X为= CH 2时，R 3和R 4各自为CF 3，A为双键，R 1或R 2中的一个为氢，则R 1或R 2中的另一个为CH 3; （ⅱ）当X为= CH2时，R3和R4分别为（C1-C2）烷基，A为双键，R2为氢，则R1不能为CH3; （iii）当X为= CH 2时，R 3和R 4各自为（C 1 -C 4）烷基，A为双键，R 1为氢，则R 2不能为CH 3; （iv）当X为= CH 2时，R 3或R 4中的一个为CF 3，A为双键，R 1为CH 3，R 2为氢，则R 3或R 4中的另一个为CH 3; 和（v）当X是（H，H）时，R 3和R 4各自是CF 3，A是双键，B是三键，R 2是氢，则R 1不能是CH 3， 其中：X为（H，H）或= CH2; R 1和R 2彼此独立地为氢，（C 1 -C 4）烷基或氟代烷基，或者R 1和R 2与C 20一起形成（C 3 -C 6）环烷基或环氟烷基，或者R 1和R 2一起形成= CH 2; R 3和R 4彼此独立地为（C 1 -C 4）烷基或氟烷基，或者R 3和R 4与C-25一起形成（C 3 -C 9）环烷基或环氟烷基; A是单键或双键; B是双键或三键; 不同之处在于R3和R4各自为CF3且A为双键，B为三键，R2为氢，则R1不能为CH3，可用于治疗骨质疏松症。 -
公开(公告)号：EP0808832B1
公开(公告)日：2003-04-23
申请号：EP97107868.8
申请日：1997-05-14
发明人： Manchand, Percy Sarwood , Nestor Jr., John Joseph , Uskokovic, Milan Radoje , Vickery, Brian Henry
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00 , C07F7/1856 , Y02P20/55
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6.发明公开Process for the manufacture of benzopyran derivatives 失效Verfahren zur Herstellung von Benzopyran-Derivaten。
公开(公告)号：EP0355617A1
公开(公告)日：1990-02-28
申请号：EP89114880.1
申请日：1989-08-11
IPC分类号： C07D311/74
CPC分类号： C07D311/66 , C07D311/58
摘要： The invention is directed to a process and intermediates for the preparation of benzopyrans such as racemic-6-acetyl-7-[5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentyloxy]-3,4-dihydro-2H-1-benzopyran-2-carboxylic acid.
摘要翻译： 本发明涉及制备苯并吡喃的方法和中间体，例如外消旋-6-乙酰基-7- [5-（4-乙酰基-3-羟基-2-丙基苯氧基）戊氧基] -3,4-二氢-2H -1-苯并吡喃-2-羧酸。
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7.发明公开Process for preparing intermediates for vitamin D derivatives and novel compounds obtained thereby 失效一种制备用于维生素D衍生物和新颖的化合物的中间体的过程。
公开(公告)号：EP0528209A1
公开(公告)日：1993-02-24
申请号：EP92112775.9
申请日：1992-07-27
IPC分类号： C07F7/18 , C07C401/00
CPC分类号： C07J9/00 , C07C401/00 , C07D333/72 , C07F7/1856 , C07F7/1892 , C07J51/00
摘要： Compounds of the formula
wherein A is a 23,24-bisnorsteroid or a 23,24-bisnor-9,10-secosteroid radical, wherein the free valence bond is in the 22-position and wherein any hydroxy groups present are protected; R₁ is hydrogen, carboxy,
lower alkoxycarbonyl, lower alkylcarbonyl or unsubstituted or substituted lower alkyl; and R₂ is hydroxyl, lower alkoxy, or unusbstituted or substituted lower alkyl,
can be prepared from compounds of formula AX wherein X is halogen, and compounds of formula
The compounds of formula IV can be converted into calcitriol and related compounds.摘要翻译： 下式的化合物
worin A为23,24-bisnorsteroid或23,24-bisnor -9,10-开环甾族化合物基团，所述worin自由价键是在22位上和羟基呈现任何worin被保护 ; R1是氢，羧基，低级烷氧基羰，低级烷基羰基或unsubstituiertem或取代的低级烷基; 且R 2是羟基，低级烷氧基，或unusbstituted或substituiertem低级烷基，可以由式AX worin X的化合物制备为卤素，和式I化合物 式IV的化合物可被转化成骨化三醇和相关化合物。 -
公开(公告)号：EP0341704A3
公开(公告)日：1990-12-05
申请号：EP89108442.8
申请日：1989-05-10
发明人： Belica, Peter Stefan , Huang, Tai-Nang , Manchand, Percy Sarwood , Partridge, John Joseph , Tam, Steve
IPC分类号： C07D405/04 , A61K31/505
CPC分类号： C07D405/04 , C07H19/06 , Y02P20/55
摘要： Die Erfindung betrifft ein Verfahren zur Herstellung von 2′,3′-Dideoxycytidin, dadurch gekennzeichnet, dass man
a) die 4-Aminogruppe von Cytidin mit einer geeigneten Schutzgruppe schützt, b) das geschützte Cytidin zum entsprechenden Bromacetatderivat bromacetyliert, c) das Bromatom und die Acetoxygruppe aus dem Bromacetat reduktiv eliminiert um das 2′,3′-Didehydroderivat zu erhalten, d) das 2′,3′-Didehydroderivat hydriert und e) aus dem so erhaltenen an der 4-Amino und 5′-Hydroxygruppe geschützten 2′,3′-Dideoxycytidin die Schutzgruppen entfernt, um 2′,3′-Dideoxycytidin zu erhalten; sowie neue in diesem Verfahren vorkommende Zwischenprodukte.-
9.发明公开
公开(公告)号：EP0341704A2
公开(公告)日：1989-11-15
申请号：EP89108442.8
申请日：1989-05-10
发明人： Belica, Peter Stefan , Huang, Tai-Nang , Manchand, Percy Sarwood , Partridge, John Joseph , Tam, Steve
IPC分类号： C07D405/04 , A61K31/505
CPC分类号： C07D405/04 , C07H19/06 , Y02P20/55
摘要： Die Erfindung betrifft ein Verfahren zur Herstellung von 2′,3′-Dideoxycytidin, dadurch gekennzeichnet, dass man
a) die 4-Aminogruppe von Cytidin mit einer geeigneten Schutzgruppe schützt,
b) das geschützte Cytidin zum entsprechenden Bromacetatderivat bromacetyliert,
c) das Bromatom und die Acetoxygruppe aus dem Bromacetat reduktiv eliminiert um das 2′,3′-Didehydroderivat zu erhalten,
d) das 2′,3′-Didehydroderivat hydriert und
e) aus dem so erhaltenen an der 4-Amino und 5′-Hydroxygruppe geschützten 2′,3′-Dideoxycytidin die Schutzgruppen entfernt, um 2′,3′-Dideoxycytidin zu erhalten;
sowie neue in diesem Verfahren vorkommende Zwischenprodukte.摘要翻译： 本发明涉及一种制备2'，3'-双脱氧胞苷的方法，其特征在于：a）胞苷的4-氨基被合适的保护基保护，b）保护的胞苷被溴乙酰化得到 相应的溴代乙酸酯衍生物，c）溴原子和乙酰氧基被还原从溴乙酸中除去以获得2'，3'-二脱氢衍生物，d）2'，3'-二脱氢衍生物被氢化和 e）保护基团从保护在4-氨基和5'-羟基上的2'，3'-二脱氧胞苷脱除，从而得到2'，3'-二脱氧胞苷;和在该过程中发生的新中间体 。
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