公开(公告)号：US3760087A

公开(公告)日：1973-09-18

申请号：US3760087D

申请日：1970-01-19

Applicant: HOFFMANN LA ROCHE

Inventor： HAJOS Z ,  PARRISH D

IPC: A23L27/20 ,  C11B9/00 ,  C11D3/50 ,  C11D9/44 ,  A61K7/00

CPC classification number: C11D9/442 ,  A23L27/2024 ,  A23L27/2028 ,  C11B9/0019 ,  C11D3/50

Abstract: The present invention comprises perfume compositions containing ethyl 2,4-dioxohexanoate.

Abstract translation: 本发明包括含有2,4-二氧代己酸乙酯的香料组合物。

公开(公告)号：US3825569A

公开(公告)日：1974-07-23

申请号：US18011571

申请日：1971-09-13

Applicant: HOFFMANN LA ROCHE

Inventor： HAJOS Z ,  OLIVETO E

IPC: C07C43/12 ,  C07C45/00 ,  C07D309/12 ,  C07D317/16 ,  C07D317/26 ,  C07D13/04

CPC classification number: C07C45/69 ,  C07C43/12 ,  C07C45/00 ,  C07C45/64 ,  C07C45/71 ,  C07C2603/16 ,  C07C2603/26 ,  C07D309/12 ,  C07D317/16 ,  C07D317/26 ,  C07C49/16 ,  C07C49/753 ,  C07C49/513 ,  C07C49/633

Abstract: METHODS FOR THE PREPARATION OF 2,3,3A,4,5,7,8,9,9AB,9BADECAHYDRO - 3AB-PRIMARY LOWER ALKYL-7-OXO-1H-BENZ(E) INDENES AND 4,4AB,4BA,5,6,7,8,8A,9,10-DECAHYDRO-8AB-PRIMARY LOWER ALKYL - 3H-PHENANTHREN-2-ONES BY CYCLIZING COMPOUNDS OF THE FORMULA
WHERE R1 IS HYDROGEN OR LOWER ALKYL; Z'' IS CARBONYL OR CH(OR2''); R2'' IS HYDROGEN, LOWER AKYL, LOWER ALKANOYL, BENZOYL, NITROBENZOYL, CARBOXY-LOWER ALKANOYL, CARBOXYBENZOYL, TRIFLUOROACETYL OR CAMPHORSULFONYL; T'' IS -C(X'')=CH-, -C(OR3)=CH- OR -Q''-CH2-; R3 IS LOWER ALKYL; X'' IS BROMINE, CHLORINE OR IODINE; Q'' IS CARBONYL, LOWER ALKYLENE DIOXY-METHYLENE, DI-(LOWER ALKOXY)-METHYLENE OR HYDROXY-METHYLENE, R4 IS LOWER PRIMARY ALKYL AND M IS AN INTEGER HAVING A VALUE OF 1 OR 2. THE COMPOUNDS OF THIS SERIES ARE USEFUL AS INTERMEDIATES IN THE SYNTHESIS OF KNOWN STEROIDS WHICH ARE PHARMACOLOGICALLY ACTIVE AS FERTILITY CONTROL AGENTS.

CH3)-)

R1-CH2-T''-CH2-CH(-CO-H)-CH

公开(公告)号：US3852331A

公开(公告)日：1974-12-03

申请号：US29807072

申请日：1972-10-16

Applicant: HOFFMANN LA ROCHE

Inventor： HAJOS Z

IPC: C07C62/26 ,  C07C62/38 ,  C07C69/00

CPC classification number: C07C62/38 ,  C07C62/26 ,  C07C2603/16

Abstract: Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula

WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 OR 2; R4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR2) and carbonyl; R8 when taken along is hydrogen; R9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R8 when taken alone is hydrogen; R9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, PHENYL-LOWER ALKYL, TETRAHYDROPYRANYL, LOWER ALKANOYL, BENZOYL, NITROBENZOYL, CARBOXY-LOWER ALKANOYL, CARBOXY-BENZOYL, TRIFLUOROACETYL AND CAMPHORSULFONYL AND REACTING THEM IN THE CASE WHERE R8 and R9 taken together are methylene or R8 is hydrogen and R9 is methylene-X with Beta keto esters and other analogs of the formula

WHEREIN R6 is selected from the group

LOWER ALKYL; R7 is lower alkyl; R15 is selected from the group consisting of oxo, lower alkylene-dioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxycarbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R25 and R26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.

Abstract translation: 已知的促孕活性甾体材料的全合成。 可以根据通过使用作为中间体选择的特定起始反应物来合成类固醇，其具有下式的双环化合物，其中M是具有1或2的值的整数; R4是氢或低级烷基; Z是低亚烷基二氧基，CH（OR 2）和羰基; 取R8时为氢; 当单独使用时，R 9为低级烷氧基羰基，芳氧基羰基，低级环烷氧基羰基，羰基卤化物，氢，羧基，甲酰基和亚甲基-X，其中X为离去基团，并且一起为亚甲基时; 条件是当Z为羰基时，当单独使用时为氢; 当单独使用时，R 9是羰基卤，氢，羧基，甲酰基和亚甲基-X，其中X是离去基团，当它们一起是亚甲基且R 2是氢时，低级烷基，低级烷氧基 - 低级烷基，苯基 - 低级烷基，四氢呋喃基， 低级烷基，苯甲酰基，硝基苯甲酰，羧基 - 低级烷基，羧基 - 苯甲酰基，三氟乙酸和环戊二烯并在其中反应。其中R8和R9一起为亚甲基或R8为氢，R9为亚甲基-X，带有β-酮酯等 式WHERE R6的类似物选自LOWER ALKYL; R7是低级烷基; R 15选自氧代，低级亚烷基 - 二氧基或（氢和低级烷氧基）; B选自低级烷氧基 - 羰基 - 亚甲基，低级 - 芳氧基 - 羰基 - 亚甲基，氰基亚甲基，低级烷基亚磺酰基 - 亚甲基，低级烷基磺酰基 - 亚甲基，R 25和R 26独立地选自氢 ，羟基和低级烷基。